半岛bd体育手机客户端 说明
生化/生理作用
Rupatadine (UR-12592) is an orally active, dual histamine H1 and platelet-activating factor (PAF) receptor antagonist (Ki(app) = 100/550 nM against pyrilamine/WEB2086 binding to guinea pig cerebellum/rabbit platelet membranes) that inhibits histamine-induced guinea pig ileum contraction (pA2 = 9.29) and PAF-induced platelet aggregation (IC50= 0.68 μM/human PRP). Rupatadine blocks histamine-/PAF-induced hypotension (ID50= 1.4/0.44 mg/kg i.v. rats) and bronchoconstriction (ID50= 113/9.6 μg/kg i.v. guinea pigs), as well as prevents mortality caused by PAF (ID50= 0.31 mg/kg i.v. or 3.0 mg/kg p.o. mice) and endotoxin (mice/rats ID50= 1.6/0.66 mg/kg i.v.)in vivo.
基本信息
经验(实验)分子式 | C26H26ClN3· C4H4O4 |
分子量 | 532.03 |
MDL编号 | MFCD00926499 |
半岛bd体育手机客户端 性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | powder |
颜色 | white to beige |
溶解性 | DMSO: 2 mg/mL, clear |
储存温度 | 2-8℃ |
InChI | 1S/C26H26ClN3.C4H4O4/c1-18-13-19(16-28-15-18)17-30-11-8-20(9-12-30)25-24-7-6-23(27)14-22(24)5-4-21-3-2-10-29-26(21)25;5-3(6)1-2-4(7)8/h2-3,6-7,10,13-16H,4-5,8-9,11-12,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+ |
InChI key | JYBLCDXVHQWMSU-WLHGVMLRSA-N |
安全信息
象形图 | |
警示用语: | Warning |
危险声明 | H302 |
预防措施声明 | P264 - P270 - P301 + P312 - P501 |
危险分类 | Acute Tox. 4 Oral |
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich