AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). IC50 value: pIC50 = 8.0 (pIC50, for P2X3) Target: P2X3/P2X2/3 receptor in vitro: AF-353 is a highly potent inhibitor of ,-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1] in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced
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化学信息
名称 | AF-353 |
Iupac 化学名称 | 2,4-PyriMidinediaMine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]- |
同义词 | AF-353 |
英文同义词 | AF-353 |
分子式 | C14H17IN4O2 |
分子量 | 400.21 |
Smile | IC=1C(=CC(=C(OC=2C(=NC(=NC2)N)N)C1)C(C)C)OC |
InChiKey | AATPYXMXFBBKFO-UHFFFAOYSA-N |
InChi | InChI=1S/C14H17IN4O2/c1-7(2)8-4-11(20-3)9(15)5-10(8)21-12-6-18-14(17)19-13(12)16/h4-7H,1-3H3,(H4,16,17,18,19) |
Cas号 | 865305-30-2 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |