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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $64 | In Stock | |
10 mg | $98 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $328 | In Stock | |
100 mg | $493 | In Stock | |
1 mL x 10 mM (in DMSO) | $80 | 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. |
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]. |
Alias | ABT 202 |
Molecular Weight | 565.57 |
Formula | C33H27NO8 |
Cas No. | 475205-49-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 47 mg/mL (83.10 mM) Ethanol: 90 mg/mL (159.13 mM) H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
Ethanol
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