LY3130481 - ≥99% , CAS No.1610802-47-5

CAS: 1610802-47-5 Cat. No.: L646771 Formula: C₁₉H₁₈N₄O₃S Peso molecolare: 382.44 PubChem CID: 74223604

QUALITÀ & PUREZZA ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Panoramica

LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC 50 of 65 nM

Form:Solid

IC50& Target:IC50：65 nM (AMPA/TARP γ-8)

Specifiche

Specifiche e purezza

≥99%

Meccanismi biochimici e fisiologici

LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC 50 of 65 nM.

Condizioni di conservazione di stoccaggio

Store at -20°C

Spedito in

Ice chest + Ice pads

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

ANTAGONIST

Purezza

≥99%

Nomi e identificatori

Isomeri SMILES

C[C@@H](C1=CC2=C(C=C1)NC(=O)S2)C3=NN(C=C3)C4=NC=C(C=C4)OCCO

PubChem CID

74223604

Peso molecolare

382.44

Obiettivi associati (umani)

GRIA1 Tclin Glutamate receptor 1 (1 Activities)

Discover Target: GRIA1

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

GRIA1 Tclin Glutamate receptor ionotropic, AMPA 1 (277 Activities)

Discover Target: GRIA1

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

CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)

Discover Target: CYP1A2

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

Obiettivi associati (non umani)

Rattus norvegicus (775804 Activities)

Explore this target

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

Brain (1 Activities)

Explore this target

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

Plasma (328 Activities)

Explore this target

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

Meccanismi d'azione

Proprietà chimiche e fisiche

• Solubilità: DMSO : 250 mg/mL (653.70 mM; Need ultrasonic)
• Peso molecolare: 382.400 g/mol
• XLogP3: 2.500
• Hydrogen Bond Donor Count: 2
• Hydrogen Bond Acceptor Count: 6
• Rotatable Bond Count: 6
• Exact Mass: 382.11 Da
• Monoisotopic Mass: 382.11 Da
• Topological Polar Surface Area: 115.000 Ų
• Heavy Atom Count: 27
• Formal Charge: 0
• Complexity: 525.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 1
• Undefined Atom Stereocenter Count: 0
• 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

Validated/tested application details are not provided for this item in the product data.

• Recommended assay types, working ranges, and positive controls: Not specified for this item; refer to CoA/Spec Sheet or request application notes from Aladdin Technical Support.

General suggestion:

• If adopting LY3130481 for a new assay, run a pilot titration with appropriate vehicle controls and, where possible, a benchmark compound to anchor dynamic range and assay sensitivity.

Biological Roles

Literature context (general, non-clinical):

• LY3130481 is described in the neuroscience research literature as a small-molecule modulator used to probe AMPA-type ionotropic glutamate receptors via interaction with specific auxiliary subunits (e.g., TARP family members). Such compounds enable dissection of synaptic transmission components in hippocampal and cortical circuits.
• Negative allosteric modulators targeting receptor–auxiliary protein interfaces are valuable to parse contributions of distinct receptor assemblies to excitatory neurotransmission. These tools aid in mapping subunit- and region-selective mechanisms without acting as competitive antagonists at the orthosteric glutamate site.
• Typical experimental paradigms include: patch-clamp recordings in heterologous expression systems co-expressing AMPA receptors with designated auxiliary subunits; ex vivo brain-slice electrophysiology to assess effects on EPSCs; and calcium/voltage imaging to capture population-level changes in excitatory drive.
• From a biochemical standpoint, selective modulators can reveal trafficking/stability roles of auxiliary proteins, shifts in channel gating kinetics (rise/decay times), and modulation of desensitization/recovery.

Important notes:

• The above reflects general literature use-cases and mechanistic insights for this class of tool compounds. It does not constitute a statement of specifications for this item, nor any medical/clinical claim.
• Always corroborate selectivity and potency under your exact expression system, temperature, recording configuration, and ionic composition, as auxiliary subunit stoichiometry and lipid composition can alter apparent pharmacology.

Buffer Applications

This product is not a buffering agent. However, it is commonly deployed in buffered systems for biological assays. Practical considerations:

• Electrophysiology buffers: Use well-defined artificial cerebrospinal fluid (aCSF) or HEPES-buffered saline. Maintain physiological pH (≈7.3–7.4) and osmolarity. Prepare compound stocks in DMSO and dilute into perfusate immediately before use; keep vehicle controls identical in solvent content.
• Imaging assays: In Ca2+ imaging, employ HEPES-buffered saline with controlled divalent cations (Ca2+, Mg2+). Confirm that any surfactants or solvents used to aid solubility do not perturb membrane excitability.
• Protein-binding effects: Serum proteins and BSA can markedly change free fraction in cell-based assays. Consider protein-free assay buffers or quantify free concentration via equilibrium dialysis if necessary.

General tips:

• Pre-warm and pre-equilibrate buffers to the experimental temperature before compound addition to avoid solubility shocks.
• Filter buffers (0.2 µm) to remove particulates that could confound optical or electrophysiological readouts.

Green Alternatives

LY3130481 functions as a specific research tool; there is no “green substitute” for its biological activity. However, greener choices can be made around formulation and handling:

Greener solvent considerations (for stock and dosing solutions):

• DMSO vs alternatives: While DMSO is widely used and relatively low in hazard, greener co-solvent systems may include water with cyclodextrin, propylene glycol, or ethanol/water blends—provided assay compatibility and compound solubility are validated.
• Minimize solvent load: Use the lowest effective final solvent percentage in assays (often ≤0.1–0.5% v/v) to reduce environmental and biological impact.
• Waste reduction: Prepare only the volume needed per session; aliquot stock solutions to avoid repeated thawing and disposal of degraded material.

Small comparison (general):

• DMSO: High solvency; excellent for stocks; typically acceptable at low % in bioassays; not volatile, easy to handle.
• Ethanol: Renewable source potential; volatile; may alter membrane/channel function at higher %; run stringent controls.
• PEG 400/propylene glycol: Useful co-solvents and vehicles; viscous; may affect viscosity/osmolality—verify assay tolerance.

Operational greening:

• Opt for glassware re-use where possible, minimize single-use plastics, and segregate organic vs aqueous waste to facilitate appropriate disposal.

Pharmaceutical Uses

No pharmacopeial status or excipient role is provided for this item. This product is supplied strictly for research use only.

Research and development context (non-clinical):

• Reference/analytical standard: Can serve as an internal or external standard in method development for LC–MS/MS bioanalysis during discovery-stage pharmacokinetic and metabolism studies, once identity/purity are established.
• Assay control: May be used as a positive/negative control in receptor pharmacology assays, where justified by internal validation and literature precedent.
• Stability studies: Useful for establishing stability-indicating methods (stress testing across pH, oxidative, thermal, and photolytic conditions) to support handling protocols.

Compliance note:

• This product is not intended for therapeutic, diagnostic, or clinical use. Any work related to drug product manufacturing, GLP/GMP studies, or human exposure requires separate qualification and sourcing pathways.

Physical Properties

Item-specific physicochemical specifications are not provided in this record.

• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Melting point / Boiling point: Not specified for this item; refer to CoA/Spec Sheet.
• Density / Refractive index: Not specified for this item; refer to CoA/Spec Sheet.
• Solubility: Not specified for this item; refer to CoA/Spec Sheet.
• LogP / pKa: Not specified for this item; refer to CoA/Spec Sheet.

General laboratory guidance (literature/practice, not item-specific):

• Small-molecule screening tools like LY3130481 are commonly prepared as concentrated stock solutions in high-boiling polar aprotic solvents (e.g., DMSO) and then diluted into assay buffers immediately before use to minimize precipitation.
• If aqueous work is required, evaluate co-solvent systems (e.g., DMSO ≤1–2% v/v in final assay, or use of solubilizing excipients) and confirm compatibility with your biological readout.
• Always perform a small-scale solubility/compatibility screen in the intended medium (ionic strength, pH, protein content) prior to scale-up.

Important: The above guidance is general. For any quantitative property or acceptance criterion, defer to the product’s CoA/Spec Sheet and your internal method validation.

Quality and Grades

Item-specific grade and purity are not provided in this record.

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

General guidance on quality for small-molecule research tools:

• For biochemical and electrophysiology assays, users typically require high chemical purity and low residual solvent/volatile impurities. Verification by HPLC/UPLC with orthogonal detection (UV/MS) is recommended.
• If UV-based assays are planned, low baseline absorbance and absence of chromophoric impurities at the assay wavelengths are important. Request UV spectra or run in-house scans.
• Trace inorganic content and water content may influence stability and formulation; Karl Fischer and residual metal screens can be considered for sensitive applications.
• If your use involves quantitative bioanalysis, establish identity/purity against a qualified reference standard (where available), and document solution stability (freeze–thaw cycles, bench-top stability, autosampler stability) under your exact conditions.

Documentation:

• For definitive lot-specific specifications (purity threshold, analytical methods, and acceptance criteria), please refer to the Certificate of Analysis/Specification Sheet provided with the shipment or available upon request.

Reaction and Applications

This product is primarily used as a research tool compound rather than as a synthetic reagent.

Applications (research context):

• Neuroscience receptor pharmacology: Employed in studies interrogating ionotropic glutamate receptor function and auxiliary subunit modulation (literature context). Typical readouts include whole-cell/patch-clamp electrophysiology, field recordings, and Ca2+ imaging.
• Target engagement and selectivity profiling: Used in heterologous expression systems or native tissues to evaluate functional selectivity vs. related receptor assemblies (literature context).
• Biochemical/biophysical assays: Can be incorporated into binding or thermal-shift-style assays to probe compound–protein interactions where applicable.

Not typically applicable:

• As a building block, catalyst, or stoichiometric reagent in organic synthesis, LY3130481 is not commonly used. If your intent is preparative chemistry, alternative reagents tailored to the transformation are recommended.

Practical tips (general):

• Prepare fresh dilutions immediately prior to assays; pre-clear solutions by gentle centrifugation if any microprecipitates form on dilution into buffer.
• Verify stability in your assay media over the measurement window (e.g., 1–4 hours), and establish vehicle-only controls to distinguish solvent from compound effects.

Reaction Conditions

Not typically applicable for preparative chemical reactions, as LY3130481 is used as a bioactive research tool rather than a reagent.

Assay preparation conditions (general, literature/practice):

• Stock solutions: Frequently prepared in anhydrous DMSO at high concentration and stored as single-use aliquots at ≤−20°C. Thaw immediately before use and dilute into pre-warmed assay buffer.
• Working concentrations: Established empirically for each assay; many ion channel/pharmacology experiments explore ranges spanning low-nanomolar to micromolar. Determine concentration–response under your exact conditions; include vehicle controls.
• Temperature: Electrophysiology and imaging can be sensitive to temperature; maintain a consistent experimental temperature (room temperature or physiological ~32–37°C) as defined by your protocol.
• Exposure time: Allow sufficient equilibration for allosteric modulators to reach steady-state effects; verify reversibility with washout where feasible.

These are general best practices; definitive, item-specific reaction or assay parameters are not specified for this product. Always optimize within your system and document solution stability over the experimental window.

Safety and Handling

Safety classifications for this specific item are not provided in this record.

• GHS Classification / Pictograms / H-Statements / Signal Word: Not specified for this item; refer to SDS.
• Intended use: For research use only. Not for human or veterinary use, drug, household, or food applications.

General safe-handling guidance (good laboratory practice):

• PPE: Laboratory coat, safety glasses, and suitable chemical-resistant gloves. Use a certified chemical fume hood to avoid inhalation of dusts/aerosols.
• Avoid: Inhalation, ingestion, skin and eye contact. Prevent generation of dust; handle solids gently.
• Storage incompatibilities: Keep away from strong oxidizers and strong acids/bases unless compatibility is verified. Segregate from foodstuffs.
• First aid (overview): If on skin/eyes, rinse with copious water for ≥15 min; remove contaminated clothing. If inhaled, move to fresh air. If ingested, rinse mouth; seek medical attention. Always follow your institution’s EHS protocols.
• Spill response: Avoid dust; collect with inert absorbent or damp disposable towels; place in a suitable waste container for disposal according to local regulations.
• Thermal/light sensitivity: Absent specific data, protect from light and heat; minimize repeated freeze–thaw of solutions.

Authoritative information: Always consult the product SDS and your institutional risk assessment before use.

Solvent Selection

Use-case oriented guidance for small-molecule tool compounds like LY3130481:

• Primary stock solvent (common practice): Dimethyl sulfoxide (DMSO) is the default for many screening libraries due to broad solvency and biological compatibility at low final percentages. Validate assay tolerance (often ≤0.1–1% v/v DMSO in the final system, assay-dependent).
• Alternative organic solvents: N,N-dimethylformamide (DMF) and ethanol can be used for stock preparation where compatible. Confirm absence of solvent artifacts in readouts (e.g., receptor modulation, fluorescence background).
• Aqueous systems: For water-based media, consider co-solvent approaches (DMSO + buffer), pH adjustment within the biologically acceptable range, or use of solubilizers (e.g., hydroxypropyl-β-cyclodextrin) after compatibility checks.
• Adsorption losses: Hydrophobic analytes may adsorb to plastics. Prefer glass vials/microinserts for low-concentration work; include minimal surfactant only if your assay allows.
• Filtration: Use low-protein-binding, low-extractable filters (PTFE or PVDF for organic-rich solutions; PES for aqueous) to remove particulates prior to quantitative assays.

Selection tips:

• Start with a small solubility screen across DMSO, DMF, EtOH, and intended buffers; observe clarity upon dilution to working concentrations. Record any precipitation over time.
• For electrophysiology, ensure solvent vehicle controls are run in parallel to quantify solvent effects on baseline channel activity.

Storage and Reconstitution

Item-specific storage and shipping:

• Storage Conditions: Store at −20°C.
• Shipped In: Ice chest + ice pads.

General best practices (research-use small molecules):

• Solid material: Keep tightly closed in the original container, desiccated, and protected from light. Allow the vial to equilibrate to room temperature in a desiccator before opening to minimize moisture condensation.
• Reconstitution: Prepare concentrated stock solutions in a suitable solvent (commonly anhydrous DMSO). Filter if needed (PTFE, 0.2 µm) to remove particulates.
• Aliquoting: Dispense single-use aliquots to avoid repeated freeze–thaw cycles. Store aliquots at −20°C or below in inert, moisture-tight vials.
• Handling of solutions: Thaw just before use; mix gently to avoid foaming. After dilution into aqueous buffers, use promptly to limit precipitation or degradation.
• Stability: Item-specific stability data are not provided; establish in-house stability (bench-top, autosampler, and freeze–thaw) under your exact conditions.

For definitive, lot-specific guidance (including any light sensitivity, humidity limits, or solution shelf-life), consult the CoA/Spec Sheet and SDS supplied with the product.

Structure and Identity

Overview: LY3130481 is supplied as a research-use small molecule in Aladdin’s small-molecule/compound library category.

• SKU: L646771
• Product Name: LY3130481
• CAS: 1610802-47-5
• PubChem CID: 74223604
• Category Path: 全部 / 可售 / 小分子和化合物库

Item-specific structure identifiers (for this catalog item):

• Molecular Formula: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular Weight: Not specified for this item; refer to CoA/Spec Sheet.
• SMILES: Not specified for this item; refer to CoA/Spec Sheet.
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.

Structural description (general, literature context):

• LY3130481 is reported in the literature as a small-molecule tool compound used in ionotropic glutamate receptor research. Detailed ring/functional-group description is not provided in this product record; consult primary literature or the CoA for definitive structure annotations.

Notes:

• For unambiguous identity confirmation in your lab, we recommend orthogonal verification (e.g., HRMS, 1H/13C NMR, and HPLC/UPLC purity profiling) against your project’s acceptance criteria.

Synthetic Utility

LY3130481 is a target-focused research tool and is not typically employed as a reagent, catalyst, or building block in synthetic organic chemistry.

• Functional group reactivity: Item-specific functional groups are not disclosed in this record; no guidance can be provided on derivatization or coupling without structural details. Refer to the CoA/Spec Sheet or primary literature if chemical modification is intended.
• Retrosynthetic value: Not generally used as a synthon in route scouting or library diversification; users seeking related chemotypes should consider de novo synthesis or SAR exploration around published scaffolds rather than modifying this material directly.

If your project involves chemical modification:

• Obtain definitive structural identifiers (SMILES/InChIKey) and confirm functionality compatible with your planned transformations (e.g., cross-couplings, amide couplings, late-stage C–H functionalization).
• Verify analytical comparability between starting material and any derivatives by LC–MS, NMR, and purity assays.

Target Specificity

Target details for this specific catalog item are not provided in the product data.

• Antigen/target name, epitope, species reactivity, and related selectivity information: Not specified for this item; refer to CoA/Spec Sheet or contact Aladdin Technical Support for any available characterization data relevant to your application.

Domande frequenti

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1610802-47-5, the molecular formula is C19H18N4O3S, and the molecular weight is 382.44 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.