PF-06446846 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-06446846 hydrochloride 是一种具有口服活性，高选择性前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 的翻译抑制剂。PF-06446846 hydrochloride 可通过诱导核糖体停在密码子 34 周围，从而抑制 PCSK9。

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochlorideinhibits PCSK9 by inducing the ribosome to stall around codon 34.

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM.

PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner and lowers total cholesterol levels.Animal Model:Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)Dosage:5, 15, and 50 mg/kg Administration:Oral gavage; daily for 14 daysResult:Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterol levels.

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1632250-50-0

C22H20CIN7O.XHCl

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (531.52 mM; 超声助溶 ) H2O 中的溶解度 : 100 mg/mL (212.61 mM; 超声助溶)

Cl.Clc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12

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(-20℃)

With Ice Pack

≥ 2 years