GSK598809 - ≥99% , CAS No.863680-45-9

CAS: 863680-45-9 Cat. No.: G651580 Fórmula: C₂₂H₂₃F₄N₅OS Peso molecular: 481.51 PubChem CID: 24743758

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pK i of 8.9.

In Vivo

Cocaine and GSK598809 each increases peak mean arterial blood pressure. Least square mean differences are significant for both doses of cocaine compared with its vehicle. Likewise, least square mean differences are significant for both doses of GSK598809 as compared with its vehicle. The experimental question of interest, that is, whether GSK598809 significantly increases cocaine effects on peak mean arterial blood pressure, is probed by a prior it tests on the means of the fitted regression model. The dose of 3 mg/kg GSK598809 significantly increases the pressor effects of 5.6 mg/kg cocaine and of 1.7 mg/kg cocaine . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:pKi: DRD3

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pK i of 8.9.

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

ANTAGONIST

Pureza

≥99%

Nombres e identificadores

Sonrisas canónicas

CC1=C(OC=N1)C2=NN=C(N2C)SCCCN3CC4CC4(C3)C5=C(C=C(C=C5)C(F)(F)F)F

IUPAC Name

5-[5-[3-[1-[2-fluoro-4-(trifluoromethyl)phenyl]-3-azabicyclo[3.1.0]hexan-3-yl]propylsulfanyl]-4-methyl-1,2,4-triazol-3-yl]-4-methyl-1,3-oxazole

InChIKey

ZKRWPAYTJMRKLJ-UHFFFAOYSA-N

INCHI

1S/C22H23F4N5OS/c1-13-18(32-12-27-13)19-28-29-20(30(19)2)33-7-3-6-31-10-15-9-21(15,11-31)16-5-4-14(8-17(16)23)22(24,25)26/h4-5,8,12,15H,3,6-7,9-11H2,1-2H3

Isómeros SMILES

CC1=C(OC=N1)C2=NN=C(N2C)SCCCN3CC4CC4(C3)C5=C(C=C(C=C5)C(F)(F)F)F

PubChem CID

24743758

Peso molecular

481.51

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • Clase Piperidines
      • Subclass Phenylpiperidines

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Clase: Piperidines
• Subclass: Phenylpiperidines
• Intermediate Tree Nodes: Not available
• Direct Parent: Phenylpiperidines
• Alternative Parents: Phenylpyrrolidines Trifluoromethylbenzenes 4,5-disubstituted oxazoles Alkylarylthioethers Aralkylamines Fluorobenzenes Aryl fluorides N-alkylpyrrolidines Heteroaromatic compounds Pyrroles Triazoles Trialkylamines Azacyclic compounds Sulfenyl compounds Oxacyclic compounds Organofluorides Alkyl fluorides Hydrocarbon derivatives Organooxygen compounds
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: Phenylpiperidine - 3-phenylpyrrolidine - Trifluoromethylbenzene - Aryl thioether - 4,5-disubstituted 1,3-oxazole - Fluorobenzene - Halobenzene - Alkylarylthioether - Aralkylamine - Benzenoid - N-alkylpyrrolidine - Aryl fluoride - Aryl halide - Monocyclic benzene moiety - Heteroaromatic compound - 1,2,4-triazole - Azole - Pyrrolidine - Pyrrole - Oxazole - Tertiary aliphatic amine - Tertiary amine - Thioether - Sulfenyl compound - Azacycle - Oxacycle - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Alkyl halide - Alkyl fluoride - Amine - Hydrocarbon derivative - Organic oxygen compound - Organic nitrogen compound - Aromatic heteropolycyclic compound
• Descripción: This compound belongs to the class of organic compounds known as phenylpiperidines. These are compounds containing a phenylpiperidine skeleton, which consists of a piperidine bound to a phenyl group.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Objetivos asociados (humanos)

DRD3 Tclin D(3) dopamine receptor (2 Activities)

Discover Target: DRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 (4 Activities)

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD2 Tclin Dopamine D2 receptor (23596 Activities)

Discover Target: DRD2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD3 Tclin Dopamine D3 receptor (14368 Activities)

Discover Target: DRD3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HRH3 Tclin Histamine H3 receptor (10389 Activities)

Discover Target: HRH3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Objetivos asociados (no humanos)

Cavia porcellus (23802 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mecanismos de acción

Propiedades químicas y físicas

• Solubilidad: DMSO : 83.33 mg/mL (173.06 mM; Need ultrasonic) 1M HCl : 28.57 mg/mL (59.33 mM; ultrasonic and adjust pH to 2 with HCl)
• Peso molecular: 481.500 g/mol
• XLogP3: 4.100
• Hydrogen Bond Donor Count: 0
• Hydrogen Bond Acceptor Count: 10
• Rotatable Bond Count: 7
• Exact Mass: 481.156 Da
• Monoisotopic Mass: 481.156 Da
• Topological Polar Surface Area: 85.300 Ų
• Heavy Atom Count: 33
• Formal Charge: 0
• Complexity: 704.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• Undefined Atom Stereocenter Count: 2
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1

Application Protocols

• Item-specific tested applications: Not specified for this item; refer to CoA/Spec Sheet.

• General protocols for small-molecule GPCR ligands (illustrative; adjust to your platform)

  • Stock preparation
    • Equilibrate vial to room temperature in a desiccator. Open under dry air or nitrogen. Dissolve to 10 mM in anhydrous DMSO. Vortex until fully dissolved. If particulates persist, brief sonication may help.
    • Aliquot into low-bind microtubes (e.g., 10–50 μL) to avoid repeated freeze–thaw. Store at −20 °C, protected from light.
  • Radioligand binding (membrane prep)
    • Prepare serial dilutions in assay buffer with constant DMSO percentage across all concentrations.
    • Incubate membranes expressing human DRD3 with a fixed concentration of [3H]-radioligand and varying concentrations of test compound (10-point, 0.1 nM–10 μM) for 60–120 min at 25 °C.
    • Separate bound/free (filtration or SPA), quantify radioactivity, and fit to competitive binding models to estimate Ki (Cheng–Prusoff correction).
  • Functional assay (cAMP)
    • Use cells stably expressing DRD3. Pre-incubate with forskolin to elevate cAMP. Add dopamine ± test compound to measure antagonism via cAMP detection kit (HTRF/ELISA).
    • Maintain vehicle control DMSO ≤0.1% and include D2-expressing counter-screen to assess selectivity.

• Quality controls

  • Include reference ligands and plate-level controls; monitor for edge effects and compound precipitation. Confirm concentration by UV or LC–MS if critical.

Biological Roles

• Literature context (not item specifications or medical claims)

  • GSK598809 has been reported as a selective dopamine D3 receptor antagonist. The D3 receptor is a D2-like GPCR predominantly expressed in limbic brain regions and is implicated in modulation of dopaminergic signaling related to motivation and reward pathways. Antagonists serve as research tools to dissect D3-specific signaling, receptor reserve, and downstream second-messenger cascades (e.g., inhibition of adenylyl cyclase via Gi/o coupling).
  • In cellular systems, D3 ligands are evaluated using assays such as radioligand binding (e.g., [3H]-spiperone displacement on D2/D3 membranes), cAMP accumulation assays in cells expressing D3, and β-arrestin recruitment. Selectivity over D2 is a key parameter to interpret pathway-specific outcomes.

• Practical research implications

  • Use as a reference antagonist to benchmark new chemical entities targeting D3 in binding and functional assays.
  • Explore receptor desensitization, internalization, and signaling bias by comparing antagonist effects across multiple readouts.
  • Incorporate appropriate vehicle controls and counter-screens for off-target GPCRs and transporters to validate specificity in complex biological systems.

• Important note

  • For research use only. No clinical, diagnostic, or therapeutic use. Always confirm the exact potency/selectivity values for the specific lot using primary literature or in-house assays before drawing biological conclusions.

Buffer Applications

This product is a bioactive small molecule used in pharmacological assays; it is not a buffering agent.

• Practical notes for assay buffers
  • Vehicle: DMSO stocks are commonly diluted into physiological buffers (e.g., HBSS, PBS, Krebs–HEPES) for cell-based or membrane assays.
  • pH considerations: If converting to a salt to enhance solubility, use volatile acids (e.g., HCl, TFA at low equivalents) and ensure final assay pH remains within physiological range (7.2–7.4) to avoid confounding receptor function.
  • Protein binding: Consider adding 0.1–0.5% BSA where protein binding and nonspecific adsorption could affect apparent potency.

For dedicated buffer systems (e.g., Tris, HEPES, MOPS), consult those reagents’ specific product pages.

Green Alternatives

Because this product is a targeted research ligand rather than a solvent or bulk reagent, “green alternatives” are generally not applicable in the usual sense. Nonetheless, greener practices can still be implemented in its handling and use:

• Solvent and dilution strategy

  • Use the minimum DMSO necessary to solubilize the compound; consider aqueous stock preparation of a defined salt (if chemically appropriate) to reduce DMSO consumption, validating stability and activity.
  • Employ micro-scale assays and miniaturization (384/1536-well formats) to reduce material and solvent use.

• Waste minimization

  • Consolidate DMSO/organic waste streams for compliant disposal; avoid unnecessary serial dilutions that become hazardous waste.
  • Plan experiments with pre-calculated dose–response ranges to minimize over-preparation of solutions.

• Packaging and storage

  • Aliquot upon first thaw to minimize repeated handling and potential degradation, thereby reducing the need for re-synthesis or re-purchase.

• Comparative note

  • For compounds where aqueous solubility is feasible via salt formation, buffered aqueous vehicles can substitute for organic co-solvents, improving EHS profiles. Confirm that such changes do not alter biological readouts.

These measures improve sustainability without altering the compound’s identity or the research outcomes.

Pharmaceutical Uses

• Scope of use

  • Supplied strictly for research use only. Not for human or veterinary use, clinical diagnosis, or as a drug substance.

• Role in pharmaceutical R&D (literature/general; not item specifications)

  • Functions as a reference or tool compound in discovery programs targeting the dopamine D3 receptor. Useful to establish assay windows, validate screening cascades, and benchmark new ligands’ potency and selectivity.
  • May be employed in formulation feasibility studies at micro-scale to evaluate solubility enhancement strategies (salt formation, co-solvents, cyclodextrins) for related chemotypes.
  • Can serve as a chromatographic/analytical reference to develop/validate LC–MS methods for D3-class ligands (retention behavior, ionization efficiency), provided authentic standards and system suitability criteria are defined.

• Regulatory note

  • No pharmacopeial monograph is implied. Any cGMP, ICH, or GLP suitability must be established independently if required by your program. Refer to the CoA for analytical controls available for this catalog item.

Physical Properties

• Item-specific data

  • Appearance: Not specified for this item; refer to CoA/Spec Sheet.
  • Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.

• Literature/general expectations for similar GPCR-targeted small molecules (not item specifications)

  • Physical state: typically a crystalline solid or amorphous solid at ambient conditions; often supplied as free base or as an HCl salt for handling. Confirm form on CoA.
  • Solubility profile: many D3 ligands are sparingly soluble in water (<1 mg/mL) as free bases but readily soluble in DMSO (10–50 mM stock solutions common) and organic solvents such as methanol or ethanol. Aqueous solubility can increase with acidification (salt formation). Measure experimentally for this lot.
  • pKa/logP: basic amine-containing ligands often show pKa ~8–10 and cLogP in the 2–5 range; exact values for GSK598809 should be taken from primary databases and experimentally verified for your application.
  • Melting point, boiling point, density, refractive index: Not specified for this item; refer to CoA/Spec Sheet. If needed, determine MP by DSC or capillary method on receipt.

• Practical notes

  • Prepare DMSO stocks under dry conditions to avoid hydration-dependent variability.
  • For aqueous assays, pre-dilute DMSO stocks into buffer with vigorous mixing and keep final DMSO ≤0.1–0.5% v/v where assay-tolerated.
  • Perform a small solubility screen (PBS pH 7.4, HBSS, assay buffer) before high-throughput use.

Quality and Grades

• Item-specific

  • Grade/purity: Not specified for this item; refer to CoA/Spec Sheet.

• What to expect for a library-grade small molecule from Aladdin Scientific

  • Identity confirmation: typically supported by 1H NMR and/or LC–MS; some lots may include 13C NMR and HRMS. Verify the provided analytical package on the CoA.
  • Purity assessment: most screening compounds are supplied with HPLC purity (UV or ELSD) and a single major peak; exact acceptance criteria vary by program (e.g., ≥95% typical for screening, ≥98% for lead optimization). This item’s exact value is Not specified; refer to CoA/Spec Sheet.
  • Counterion/form: many basic ligands are provided as free bases or hydrochloride salts; form influences solubility and assay behavior. Confirm salt form and residual solvent levels on the CoA.
  • Impurity considerations: residual solvents and inorganic salts may be present at trace levels depending on final isolation. Water content and specific impurity limits are Not specified for this item; refer to CoA/Spec Sheet.

• Practical QC recommendations (user-side)

  • Upon receipt, record lot number and request CoA.
  • Verify purity by analytical HPLC (two orthogonal methods if possible) and confirm mass by LC–MS for critical experiments.
  • For hit-validation work, consider re-purification or re-crystallization and full NMR characterization to eliminate PAINS/artefacts.

Reaction and Applications

This product is sold as a bioactive small molecule for research and screening; it is not primarily intended as a synthetic reagent. Accordingly, classical synthetic “reaction applications” are limited.

• Research and screening applications (literature/general)

  • Target class: G protein–coupled receptor (GPCR) ligand, reported in the literature as a selective dopamine D3 receptor antagonist probe. Suitable for target engagement studies, receptor binding assays, and phenotypic screening where D3 pathways are implicated.
  • Assay modalities: radioligand binding (Ki determination), functional assays (cAMP accumulation, β-arrestin recruitment), and selectivity panels against D2-like receptors. Implement counter-screens to rule out non-specific effects.
  • SAR/chemistry enablement: can serve as a reference compound in medicinal chemistry campaigns to benchmark potency and selectivity.

• Practical usage tips

  • Prepare fresh DMSO stocks and store aliquots at −20 °C protected from light. Avoid repeated freeze–thaw.
  • Confirm identity/purity prior to use in quantitative pharmacology (e.g., Cheng–Prusoff analyses) to ensure accurate potency estimates.
  • Verify absence of assay interference (fluorescence/absorbance overlap) in optical readouts; perform interference controls as per your platform.

• Not a catalyst/reagent

  • This item is not typically used as a reagent/catalyst in synthetic organic transformations. For synthetic chemistry guidance, see the “Synthetic Utility” and “Reaction Conditions” tabs (limited applicability).

Reaction Conditions

Not directly applicable: this product is a finished small-molecule research ligand, not a reagent or catalyst.

• If pursuing analog synthesis (literature/general guidance, not item specifications)

  • Typical bond constructions for related scaffolds include: aryl–aryl or aryl–heteroaryl couplings (Suzuki–Miyaura: Pd(0/II) catalysts, 60–100 °C, aqueous organic solvents); nucleophilic substitutions on activated heteroarenes (DMF/DMSO, 25–100 °C); reductive aminations to append dialkylamino side chains (NaBH3CN or H2/Pd, 0–25 °C); amide/urea formations (carbodiimide or CDI reagents, 0–25 °C).
  • Purification often relies on reverse-phase prep HPLC due to basic, lipophilic character; salt formation (e.g., HCl) can aid crystallization.

• Assay preparation conditions (practical use)

  • Stock solutions: 10–50 mM in anhydrous DMSO, aliquoted and stored at −20 °C, protected from light.
  • Working solutions: prepare fresh on the day of use; final DMSO in assay commonly ≤0.1–0.5% v/v. Verify compound stability over the assay duration (up to 24–48 h) by LC–MS if results are sensitive to degradation.

Safety and Handling

• Regulatory and hazard information (item-specific)

  • GHS classification: Not specified for this item; refer to SDS.
  • Signal word / H-statements / Pictograms: Not specified for this item; refer to SDS.

• General laboratory safety guidance for research small molecules

  • Handle in a chemical fume hood while wearing appropriate PPE: lab coat, safety glasses, and disposable nitrile gloves. Avoid inhalation of dusts or aerosols and skin/eye contact.
  • Avoid generating dust; use antistatic measures and weigh using a draft-free enclosure if available.
  • Incompatibilities: strong oxidizers, strong acids/bases may degrade amine/heteroaromatic scaffolds; avoid prolonged exposure to light and moisture which can promote decomposition.
  • First aid (overview; consult SDS for details):
    • Inhalation: move to fresh air; seek medical attention if symptoms persist.
    • Skin contact: wash with soap and water; remove contaminated clothing.
    • Eye contact: rinse cautiously with water for several minutes; remove contact lenses if present and easy to do; seek medical attention for irritation.
    • Ingestion: rinse mouth; do not induce vomiting; seek medical attention.
  • Spill response: avoid dust formation, collect with inert absorbent, place in a suitable waste container for disposal per institutional protocols.

• Special risks/notes

  • Bioactivity: treat as a potent pharmacological agent; minimize exposure and avoid environmental release.
  • Always defer to the product SDS and your institution’s EHS guidance for authoritative hazard classifications and exposure controls.

Solvent Selection

• Primary preparation solvent (typical for bioactive small molecules; literature/common practice)

  • DMSO: preferred for making concentrated stock solutions (e.g., 10–50 mM) due to broad solvating power and stability. Filter-sterilize if needed (0.2 μm PTFE) and aliquot to minimize freeze–thaw.

• Alternative solvents (as applicable)

  • Methanol or ethanol: suitable for intermediate dilutions; verify assay compatibility.
  • Aqueous buffers: limited direct solubility expected for neutral/free-base forms; increase solubility by forming salts (e.g., dilute HCl) or by co-solvents (≤0.5–1% DMSO) and surfactants (e.g., 0.01% Tween-80) if assay permits.
  • PEG400 or propylene glycol: options for higher-concentration stocks in formulation studies; viscosity and assay interference must be evaluated.

• Polarity and miscibility (general)

  • As a drug-like heteroatom-containing ligand, the compound is amphiphilic with likely basic functionality; it is generally miscible with polar aprotic organics and co-solvent systems but has limited water solubility as the free base.

• Practical selection guidance

  • Choose DMSO for master stocks, then perform serial dilutions into the final assay buffer, ensuring vigorous mixing to prevent precipitation.
  • Pre-screen solubility at target working concentrations across your assay temperature and ionic strength. Monitor for precipitation or adsorption to plastics.
  • Minimize DMSO carryover to avoid GPCR assay artifacts; include vehicle controls matching the highest DMSO concentration used.

Storage and Reconstitution

• Item-specific storage and shipping

  • Storage conditions: Store at −20 °C (per Product Data).
  • Shipped in: Ice chest + ice pads.

• Reconstitution guidelines (general best practices for small molecules)

  • Upon arrival, allow the sealed container to equilibrate to room temperature before opening to prevent moisture condensation.
  • If provided as a solid: dissolve in anhydrous DMSO to prepare a 10–50 mM stock. Mix thoroughly (vortex/sonicate). If provided as a solution, verify concentration on the label/CoA.
  • Aliquot the stock into small, single-use portions in low-bind tubes. Protect from light if the scaffold contains chromophores susceptible to photodegradation.
  • Freeze at −20 °C or below. Avoid repeated freeze–thaw cycles; thaw on ice or at room temperature just before use.

• Stability and precautions

  • Long-term stability, water content, and specific degradation pathways: Not specified for this item; refer to CoA/Spec Sheet and SDS.
  • For aqueous working solutions, prepare fresh on the day of use. If extended stability is required, verify by analytical HPLC/LC–MS under your buffer conditions.
  • Label aliquots with compound name, concentration, solvent, date, and lot number to maintain traceability.

• Research use note

  • For research use only. Not for human or veterinary use.

Structure and Identity

Brief description: GSK598809 is a cataloged small molecule in our “Small-Molecule & Compound Libraries” category, supplied for research use.

• Item-specific (from Product Data)

  • Product name: GSK598809 (SKU: G651580)
  • CAS: 863680-45-9
  • PubChem CID: 24743758
  • InChIKey (as provided): 459635
  • SMILES: Not specified for this item; refer to CoA/Spec Sheet.
  • Molecular formula: Not specified for this item; refer to CoA/Spec Sheet.
  • Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.

• Literature/General identity notes (for context; not item specifications)

  • Compound class: drug-like, CNS-directed research tool reported in the literature as a selective dopamine D3 receptor ligand/antagonist candidate (GPCR-targeted). Consult primary literature and PubChem CID 24743758 for canonical SMILES/InChI.
  • Structural features (literature): multi-ring, heteroatom-containing scaffold typical of GPCR ligands; basic tertiary amine functionality is commonly present in D2/D3 ligands, often necessitating salt formation for solubility. Verify actual functional groups on the CoA.
  • 2D description (generic/literature): polycyclic aromatic/heteroaromatic core linked to a basic side chain; potential H-bond acceptors (heteroatoms) and donors depending on exact substitution. Exact positions and stereochemistry must be confirmed from authoritative databases.

• Best practice

  • For unambiguous identification in your records, cross-reference the CAS and CID above with your in-house registry and request the current CoA/Spec Sheet for the exact structure string (SMILES) and analytical identity data (NMR, HRMS).

Synthetic Utility

This item is supplied as a finished bioactive small molecule and is not typically used as a synthetic building block.

• General medicinal chemistry perspectives (literature/general)

  • GPCR dopamine D3 ligands often feature: (i) a basic amine tethered to (ii) a polycyclic/heteroaromatic pharmacophore with (iii) H-bond acceptors/donors positioned for D3 pocket interactions. Such scaffolds inform retrosynthetic analysis for analogue design (e.g., late-stage amide/urea formation, O-alkylation/ether linkages, Buchwald–Hartwig or SNAr on heteroaryl cores).
  • If analog generation is intended, common disconnections include: cleavage of the basic side chain from the aromatic core (installed via N-alkylation or reductive amination) and modular variation of substituents via cross-coupling (Suzuki–Miyaura) or nucleophilic aromatic substitution on activated heteroaryl systems.

• Practical note

  • For chemical synthesis applications, consult primary literature on GSK598809 scaffold synthesis for protecting-group strategies, chiral induction/resolution (if stereocenters are present), and scalable coupling conditions. These are not provided as specifications for this catalog item.

Target Specificity

• Item-specific

  • No target specificity is specified in the product data.

• Literature context (for user orientation; not a specification)

  • GSK598809 is reported as a selective antagonist of the dopamine D3 receptor (DRD3), with attention to selectivity over the closely related D2 receptor. Exact Ki/IC50 values, species differences, and assay formats vary by source; consult primary literature and verify in-house.

• Recommendations

  • When employing this compound as a D3 reference tool, run parallel assays versus D2 and other D2-like receptors, and include orthogonal readouts (binding vs. function) to confirm specificity under your experimental conditions.