PF-06815345

产品名称：

2334434-49-8
PF-06815345
(1S)-1-(5-(4-(4-((3-Chloropyridin-2-yl)((R)-piperidin-3-yl)carbamoyl)-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl)-1H-tetrazol-1-yl)ethyl ethyl carbonate hydrochloride
PF 06815345
PF06815345
Ethyl (S)-1-{5-[4-(4-{(3-chloropyridin-2-yl)[(3R)-piperidin-3-yl]carbamoyl}-2-fluorophenyl)-1-methyl-1H-pyrazol-5-yl]-1H-tetrazol-1-yl}ethyl carbonate hydrochloride

产品介绍：

产品说明

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 by in vitro hPCSK9 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 monkeys in 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

产品性质

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