Farampator - Moligand™, 10 mM in DMSO , CAS No.211735-76-1

CAS: 211735-76-1 Cat. No.: F1494305 Summenformel: C₁₂H₁₃N₃O₂ Molekulargewicht: 231.25

QUALITÄT & REINHEIT Moligand™, 10 mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Farampator (CX-691;Org24448) is an AMPA receptor positive modulator.

Spezifikationen

Spezifikationen & Reinheit

Moligand™, 10 mM in DMSO

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

MODULATOR

Produkteigenschaften

ALogP

1.5

Namen und Kennungen

Isomere SMILES

C1CCN(CC1)C(=O)C2=CC3=NON=C3C=C2

Molekulargewicht

231.25

Reaxy-Rn

13677286

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13677286&ln=

Application Protocols

General, non-item-specific protocols for small-molecule screening compounds. Adjust based on your assay and confirm solubility/stability for this lot.

• Stock preparation:

  • Dissolve compound in anhydrous DMSO to 10–50 mM. Vortex/sonicate briefly; avoid prolonged heating. Filter only if necessary and compatible.
  • Aliquot into low-bind, amber vials/plates; store at -80°C.

• Working solutions:

  • Prepare intermediate dilutions in DMSO (e.g., 100×) to minimize aqueous precipitation on final dilution.
  • Add to assay buffer/cell media to reach desired final concentration with ≤0.1–1% DMSO.

• Electrophysiology (illustrative):

  • Prepare fresh working solution immediately before recording. Apply with rapid perfusion systems; include vehicle control. Monitor series resistance and rundown; perform washout to assess reversibility.

• Biochemical assays:

  • For receptor modulation assays, pre-incubate compound with the receptor preparation if protocol requires. Include multiple concentrations (≥8-point dose–response). Use duplicate/triplicate wells and independent repeats.

• Data quality controls:

  • Include vehicle-only, positive control (if available), and matrix controls. Track well position effects and potential adsorption to plastics.

• Documentation:

  • Record lot number, exact solvent composition, and storage history for reproducibility.

Biological Roles

Research context (literature, not item-specific claims):

• Farampator is reported in the literature as an “ampakine,” a positive allosteric modulator of AMPA-type ionotropic glutamate receptors. Such compounds are used as tool molecules to probe synaptic transmission, plasticity, and excitatory signaling pathways in neurons.
• As a PAM, the compound class typically increases receptor responsiveness to endogenous glutamate without directly activating the receptor, enabling nuanced studies of receptor kinetics, desensitization, and network-level excitability.

Experimental utility (general guidance):

• Electrophysiology: Whole-cell patch clamp or field EPSP recordings to quantify changes in AMPA receptor-mediated currents.
• Biochemistry/biophysics: Radioligand displacement, fluorescence-based binding, and thermal shift assays to evaluate binding cooperativity with agonists.
• Cellular assays: Ca2+ imaging or reporter assays in cultured neurons or recombinant systems expressing AMPA subunits (GluA1–GluA4), with careful control of vehicle and exposure times.

Caveats:

• AMPA receptor modulation can alter excitability; establish concentration–effect relationships and include washout studies. Verify off-target profiles where possible (e.g., NMDA, kainate receptors) to interpret results correctly.
• Ensure that conclusions are made within the scope of research use; no claims are made for diagnostic or therapeutic applications.

Buffer Applications

This product is a small-molecule screening ligand and is not a buffering reagent.

• Not typically used to prepare buffer systems or maintain pH.
• For biological assays, prepare buffers (e.g., HEPES-, phosphate-, or bicarbonate-based) appropriate to the biological system, then add Farampator from a DMSO stock solution to the final working concentration, keeping DMSO ≤1% v/v.
• Confirm compound stability in the chosen buffer over the assay timeframe (short-term bench stability and light sensitivity).

Green Alternatives

Although Farampator is a specialty screening ligand rather than a solvent or bulk reagent, greener choices still apply to its handling and analytics.

• Solvent choices (general greener hierarchy):
  • Prefer ethanol or isopropanol over methanol where analytically feasible (lower toxicity), and acetonitrile over dichloromethane for chromatography when resolution permits.
  • Use water-rich mobile phases and volatile buffers (ammonium formate/acetate) to reduce persistence.
• Stock solutions:
  • Minimize DMSO volumes by preparing higher-concentration master stocks and aliquoting to reduce waste. Consider 96-well aliquots to curb repeated freeze–thaw.
• Scale minimization:
  • Adopt microplate-based assays and microscale analytics (UPLC, microflow LC–MS) to reduce solvent consumption.

Trade-offs:

• While DMSO is not the greenest solvent, it is often indispensable for hydrophobic ligands; mitigate by using minimal volumes and robust waste segregation.
• Acetonitrile shortages may necessitate methanol substitution; evaluate separation efficiency and ionization trade-offs.

Sustainable practices:

• Use amber glass vials to extend solution life and decrease re-preparation frequency.
• Consolidate courier shipments on dry ice to reduce logistic footprint while preserving required cold chain.

Pharmaceutical Uses

Formulation/manufacturing context (general; no therapeutic claims):

• Supplied as a research-use-only small molecule in the Moligand™ library; not intended as an API, excipient, or for GMP manufacturing.
• There is no pharmacopeial monograph known for this item within this catalog entry.

Experimental formulation guidance (research setting):

• Prepare concentrated DMSO stocks for in vitro studies and, if applicable to nonclinical enabling work, evaluate co-solvent systems (e.g., PEG400, ethanol, Cremophor EL, Captisol) only within approved institutional protocols.
• Assess adsorption to plastics and stability upon dilution into aqueous media or serum-containing matrices. Employ low-bind tubes/plates and protect from light as needed.

Regulatory note:

• For research use only. Not for human or veterinary use, not for diagnostic procedures, and not for ex vivo clinical applications.

Physical Properties

Item-specific specifications:

• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular weight: Not specified for this item; refer to CoA/Spec Sheet.
• Melting point, boiling point, density, refractive index, pKa, logP/logD, solubility in common solvents: Not specified for this item; refer to CoA/Spec Sheet.

Literature/general notes (for planning only; verify against primary data prior to use):

• Small-molecule screening ligands of this class are often solids at ambient conditions and are commonly prepared as DMSO stock solutions for biochemical and cell-based assays due to limited aqueous solubility. Final aqueous assay concentrations typically include 0.1–1% v/v DMSO to ensure solubilization while minimizing vehicle effects.
• If a UV-based quantification is intended, first obtain the exact structure and record a measured UV–Vis spectrum to determine the actual λmax and ε; do not assume class-typical values.

Practical guidance:

• Perform a small-scale solubility screen (e.g., DMSO, DMF, ethanol, PBS with 0.5–2% DMSO, and cell culture media with carrier protein) to establish reliable working concentrations.
• If crystalline, a gentle 30–40°C warm bath and vortex/sonication can assist dissolution in anhydrous DMSO; avoid prolonged heating.
• Use 0.22 µm filtration for sterile applications only after confirming no significant loss to filters (pre-rinse with vehicle).

Quality and Grades

• Grade/Purity: Moligand™ (item-specific)

What Moligand™ implies (general description):

• Moligand™ denotes a screening-grade small-molecule intended for ligand discovery, target validation, and SAR exploration. Emphasis is typically on structural identity and practical assay suitability rather than ultra-trace impurity control for manufacturing.
• UV background, trace metals, water/peroxide content, and salt form specifics are not specified for this item; refer to CoA/Spec Sheet for lot-level details.

How to use Moligand™ materials effectively:

• Identity/purity verification: For critical studies, confirm by orthogonal methods (e.g., LC–MS with exact mass, 1H NMR integration, HPLC/UPLC purity). Record the salt form and hydration/solvate state when calculating molarity.
• Assay readiness: Prepare DMSO master stocks and perform a quick stability check (24–72 h at room temperature and 4°C in assay buffer with vehicle) before committing to screening campaigns.
• Impurity awareness: Trace impurities may confound bioassays at low micromolar concentrations. Run vehicle and “depleted” controls (e.g., solid-phase cleanup or charcoal-stripped media) if potency shifts are suspected.

When to request higher specification:

• For quantitative biophysics (ITC, SPR) or in vivo enabling studies, consider higher-purity material, definitive salt form assignment, and comprehensive CoA (residual solvents, water, counterions).

Reaction and Applications

This product is supplied as a ready-to-use screening ligand and is not typically employed as a synthetic reagent or catalyst.

Applicable uses (research context):

• Tool compound use in receptor/ion-channel pharmacology, biophysics, and electrophysiology assays (literature context for the class); see Biological Roles for general notes.
• Reference control in SAR studies and cheminformatics benchmarking, once the exact structure and purity are verified for the lot.

Not typically applicable:

• As a coupling partner, reagent, or monomer in preparative organic synthesis. If derivatization is required for probe development (e.g., biotinylation, fluorophore conjugation), consult confirmed structural information and perform route scouting based on actual functional groups.

Practical tips (general):

• Establish a robust dosing workflow: DMSO master stock, intermediate plate at 100× target concentration, final assay vehicle ≤1% DMSO.
• For patch-clamp or fast ligand application studies, pre-warm and filter vehicle to minimize bubbles and adsorption; validate that the compound does not adhere to tubing or plasticware (use low-bind materials).

Reaction Conditions

Not typically applicable. Farampator is provided as a screening compound, not as a reagent or catalyst.

If chemical modification is undertaken for research probes (only after confirming exact structure):

• Perform late-stage functionalization under mild conditions to preserve the heteroaromatic core and avoid decomposition.
• Typical solvent systems for small-molecule derivatization include DMF, DMSO, MeCN, or dioxane with base/coupling reagents appropriate to the functional groups present (e.g., HATU/DIPEA for amide couplings). Reaction temperatures are often kept at ambient to 60°C to protect sensitive motifs.
• Always run analytical TLC/LC–MS time courses and small-scale trials first; scale only after stability is confirmed.

No specific yields, catalysts, or temperatures are provided for this item; consult primary literature once the definitive structure is confirmed.

Safety and Handling

Hazard designations for this specific item:

• GHS Classification: Not specified for this item; refer to SDS.
• Signal Word / Pictograms / H-Statements: Not specified for this item; refer to SDS.

General laboratory safety guidance (research use only):

• Handle in a chemical fume hood; avoid inhalation of dust/aerosols and skin/eye contact. Use appropriate PPE: lab coat, nitrile gloves, safety glasses.
• Prevent environmental release; collect waste in halogenated or non-halogenated organic waste as appropriate for the chosen solvent system.
• Given the -80°C storage requirement, minimize freeze–thaw cycles; warm sealed containers to ambient before opening to prevent condensation ingress.

First-aid overview (non-exhaustive; defer to SDS):

• Inhalation: Move to fresh air; seek medical attention if symptoms occur.
• Skin: Wash with soap and water; remove contaminated clothing.
• Eyes: Rinse cautiously with water for several minutes; remove contacts if present and easy to do.
• Ingestion: Rinse mouth; seek medical attention.

Incompatibilities and stability (general):

• Avoid strong oxidizers and strong acids/bases unless stability is known.
• Protect from light and moisture until stability data are verified for this lot.
• For DMSO solutions, use amber vials and store aliquots frozen; check for precipitation upon thawing.

Always consult the official SDS for authoritative hazard, toxicological, and disposal information for this SKU/lot.

Solvent Selection

Given the lack of item-specific solubility data, select solvents based on common practices for hydrophobic screening ligands.

• Primary stock solvent (general best practice):
  • DMSO (anhydrous) is typically preferred due to broad solubilizing power and assay compatibility at 0.1–1% v/v in aqueous systems.
• Secondary solvents for method development:
  • DMF or NMP for difficult solubilization (not usually used directly in bioassays, but useful for intermediate concentrate preparation before dilution into DMSO).
  • Ethanol or methanol for analytical sample prep when LC–MS methods prefer MeOH/MeCN systems.
• Chromatography solvents:
  • Reversed-phase LC: Water/MeCN or Water/MeOH with 0.1% formic acid or ammonium buffers. Optimize based on observed retention and ionization.

Miscibility/polarity notes (general):

• DMSO is fully miscible with water and most organics, enabling straightforward serial dilutions. Confirm absence of precipitation when diluting into high-water content buffers.

Comparison guidance (general):

• DMSO vs DMF: DMSO is more assay-compatible; choose DMF only when DMSO fails to dissolve the compound adequately.
• MeOH vs EtOH for analytics: MeOH often yields sharper LC–MS peaks but may enhance ion suppression; evaluate both.

Always verify actual solubility and stability of this lot in the intended solvent system prior to screening or quantitation.

Storage and Reconstitution

Item-specific storage and shipping:

• Storage Conditions: Store at -80°C (as provided in product data).
• Shipped In: Dry ice packs + Cold packs (as provided in product data). Maintain cold chain upon receipt.

General handling and reconstitution guidance:

• Upon arrival, inspect packaging integrity. Immediately transfer to -80°C. Avoid unnecessary freeze–thaw cycles by preparing single-use aliquots.
• Reconstitution solvent: In the absence of item-specific solubility data, anhydrous DMSO is recommended for initial dissolution. Start at 10–50 mM, adjusting based on observed solubility. Document actual concentration.
• Aliquoting: Dispense into amber, low-bind microvials/plates under dry conditions. Flush headspace with inert gas if long-term storage is planned.
• Thawing: Warm sealed vials to ambient temperature before opening to prevent moisture condensation. Mix gently after thaw; check for precipitation or turbidity.
• Stability checks: Verify short-term stability of DMSO stocks at room temperature and 4°C over the intended assay period. Reassess potency after multiple freeze–thaw events.

Specifications not provided for this item (refer to CoA/Spec Sheet): appearance, molecular weight, water content, residual solvents, and salt form.

Research use only. Not for human or veterinary use.

Structure and Identity

Brief overview: Farampator (SKU F1494305) is supplied as a research-use-only small-molecule library member under the Moligand™ line.

• CAS: 211735-76-1
• PubChem CID: 4118151 (literature identifier)
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.
• 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.

Structural features (general/literature context):

• Farampator is reported in the literature as a heteroaromatic small molecule in the “ampakine” class (positive allosteric modulators of AMPA-type ionotropic glutamate receptors). Exact atom-level representation should be confirmed from a primary structure source (e.g., SDS/CoA or PubChem) prior to quantitative work.
• Typical features in this class include fused aromatic/heteroaromatic rings and polarizable heteroatoms that support receptor binding; verify for this item before modeling, docking, or analytical method development.

2D description (general guidance):

• Planar-to-subplanar aromatic core with heteroatom functionality is commonly depicted for compounds in this class; confirm exact substitution pattern from an authoritative structure record before preparing standards, calculating extinction coefficients, or setting up purity assays.

Identity best practice:

• Cross-verify CAS and vendor lot number against a trusted database (PubChem CID 4118151) and the Aladdin CoA to lock down the definitive structure and molar mass prior to molarity-based dosing or LC–MS method setup.

Synthetic Utility

This material is supplied as a finished small-molecule ligand for screening and is not generally used as a synthetic building block.

• Because the exact functional group set for this lot is not provided here, no reaction planning should be based on assumptions. If derivatization (e.g., for probe development, photoaffinity labeling, or linker installation) is desired, first confirm the definitive structure and perform functional group compatibility scouting.

General guidance for probe derivatization (contingent on verified structure):

• Map positions tolerant to substitution using literature SAR where available; avoid perturbing the core pharmacophore essential for AMPA receptor modulation (literature context for class behavior).
• Choose chemistries compatible with the heteroaromatic core once confirmed (e.g., mild amide couplings, SNAr on activated aryl positions, or late-stage O/N-alkylation if functional handles exist), and validate bioactivity retention after modification.

Analytical considerations:

• LC–MS and 1H/13C NMR confirmation of any derivatives is essential; include purity assessment and counterion/solvate determination prior to biological testing.

Target Specificity

Only item-specific details may be listed here.

• Target, epitope, clone/isotype, or species reactivity: Not specified for this item; refer to CoA/Spec Sheet.

Note: Literature commonly discusses Farampator within the context of AMPA receptor modulation; however, this section intentionally omits literature claims and lists only product-specific information. See Biological Roles for general literature context.