半岛bd体育手机客户端 说明
生化/生理作用
PF-06815345 is a liver-targeted, orally available prodrug, which is converted by liver carboxyesterase (CES1) to its zwitterionic active drug (liver active drug = 33.9 μg/mL in mice 0.5 hr post 300 mg/kg p.o. and 9.0 μg/mL in monkeys 0.5 hr post 30 mg/kg p.o.) that selectively inhibits PCSK9 protein synthesis (IC50= 3.7 μM byin vitrohPCSK9 translation; 4.95/3.81/21/24/>27-fold selective over CDH1/HSD17B11/PCBP2/RPL27/BCAP31). PF-06815345 effectively lowers plasma PCSK9 in humanized PCSK9 mice (by 26/42/53% 5 hrs post 100/300/500 mg/kg p.o.) and is well tolerated in rats and monkeysin vivo. Note: PF-06815345 is not active in non-humanized mice.
法律信息
Sold for research purposes under agreement from Pfizer Inc.
基本信息
| 经验(实验)分子式 | C27H29ClFN9O4·HCl |
| 分子量 | 634.49 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 旋光性 | [α]/D -34 to -43°, c = 0.3 in methanol |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | room temp |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
