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A-317491 (ABT 202) 是选择性和非核苷酸的 P2X3和 P2X2/3受体的拮抗剂,通过阻断 P2X3和 P2X2/3受体介导的钙通量减轻炎性和神经性疼痛。它对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性,IC50大于10 μM。
A-317491 (ABT 202) 是选择性和非核苷酸的 P2X3和 P2X2/3受体的拮抗剂,通过阻断 P2X3和 P2X2/3受体介导的钙通量减轻炎性和神经性疼痛。它对其他 P2 受体和神经递质受体,离子通道以及酶具有高度选择性,IC50大于10 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 283 | 现货 | |
5 mg | ¥ 662 | 现货 | |
10 mg | ¥ 1,060 | 现货 | |
25 mg | ¥ 1,750 | 现货 | |
50 mg | ¥ 2,580 | 现货 | |
100 mg | ¥ 3,720 | 现货 | |
500 mg | ¥ 7,830 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 823 | 现货 |
产品描述 | 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. |
靶点活性 | P2X2:9 nM (Ki, cell free), P2X3:22 nM(Ki, cell free) |
体外活性 | 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]. |
体内活性 | 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]. |
别名 | ABT 202 |
分子量 | 565.57 |
分子式 | 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 |
密度 | 1.46 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 47 mg/mL (83.10 mM) Ethanol: 90 mg/mL (159.13 mM) H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
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