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A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $31 | In Stock | In Stock | |
| 5 mg | $64 | In Stock | In Stock | |
| 10 mg | $98 | In Stock | In Stock | |
| 25 mg | $198 | In Stock | In Stock | |
| 50 mg | $328 | In Stock | In Stock | |
| 100 mg | $493 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $80 | In Stock | In Stock |
| Description | A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors. |
| Targets&IC50 | P2X2:9 nM (Ki, cell free), P2X3:22 nM(Ki, cell free) |
| In vitro | A-317491 blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly selective (IC50 >10 μM) over other P2 receptors and other ion channels, neurotransmitter receptors, and enzymes [1]. |
| In vivo | A-317491 dose-dependently reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat (ED50: 30 μmol/kg s.c.). A-317491 is most potent in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury (ED50: 10-15 μmol/kg s.c.). Although active in chronic pain models, A-317491 is ineffective in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain (ED50 >100 μmol/kg s.c.) [1]. A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically [2]. |
| Synonyms | ABT 202 |
| Molecular Weight | 565.57 |
| Formula | C33H27NO8 |
| Cas No. | 475205-49-3 |
| Smiles | OC(=O)c1cc(C(O)=O)c(cc1C(O)=O)C(=O)N(Cc1cccc(Oc2ccccc2)c1)[C@H]1CCCc2ccccc12 |
| Relative Density. | 1.46 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 47 mg/mL (83.1 mM), Sonication is recommended. Ethanol: 90 mg/mL (159.13 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.54 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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