| CAS NO: | 475205-49-3 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 565.57 |
|---|---|
| Formula | C33H27NO8 |
| CAS No. | 475205-49-3 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL (176.81 mM) |
| Water: <1 mg/mL | |
| Ethanol: 100 mg/mL (176.81 mM) | |
| SMILES | O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C 1C(O)=O)O |
| Synonyms | A-317491; A317491; A 317491 |
| In Vitro | In vitro activity: A-317491 does not undergo any detectable metabolism (oxidation or glucuronidation) in in vitro assays using human and rat liver microsomes. It potently 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 neurotransmitter receptors, ion channels, and enzymes. Kinase Assay: A-317491 is a non-nucleotide P2X3 and P2X2/3 receptor antagonist, which inhibits calcium flux mediated by the receptors. It is known that P2X3 and P2X2/3 receptors stimulate the pronociceptive effects of ATP upon activation. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management. Cell Assay: |
|---|---|
| In Vivo | A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically. It dose-dependently (ED50 = 30 μmol/kg s.c.) reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat. A-317491 is most potent (ED50 = 10-15 μmol/kg s.c.) in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury. Although active in chronic pain models, A-317491 is ineffective (ED50>100 μmol/kg s.c.) in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain. Preliminary pharmacokinetic studies in rats indicate that 10 μmol/kg A-317491 had high (≈80%) systemic bioavailability after s.c. dosing (estimated plasma concentration = 15 μg/ml,>99% protein bound) and a half-life in plasma of 11 h. |
| Animal model | male Sprague-Dawley rats |
| Formulation & Dosage | 0.01M PBS; 3, 10 and 30 mg/kg; s.c. |
| References | Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84; Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. |
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