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PF-06446846 hydrochloride 是一种口服活性高、高选择性PCSK9(前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型)翻译抑制剂。它通过在密码子34附近诱导核糖体暂停来抑制PCSK9。

PF-06446846 hydrochloride 是一种口服活性高、高选择性PCSK9(前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型)翻译抑制剂。它通过在密码子34附近诱导核糖体暂停来抑制PCSK9。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 463 | 现货 | |
| 5 mg | ¥ 1,160 | 现货 | |
| 10 mg | ¥ 1,850 | 现货 | |
| 25 mg | ¥ 3,130 | 现货 | |
| 50 mg | ¥ 4,490 | 现货 | |
| 100 mg | ¥ 6,330 | 现货 | |
| 200 mg | ¥ 8,530 | 现货 |
| 产品描述 | PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression. |
| 体外活性 | PF-06446846 suppresses the secretion of PCSK9 by Huh7 cells (IC50: 0.3 μM)[1]. |
| 体内活性 | PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner. It also decreases total cholesterol levels[1]. |
| 分子式 | C22H20CIN7O.XHCl |
| CAS No. | 1632250-50-0 |
| Smiles | Cl.Clc1cccnc1N([C@@H]1CCCNC1)C(=O)c1ccc(cc1)-n1nnc2cccnc12 |
| 密度 | no data available |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度信息 | H2O: 90.0 mg/mL (191.3 mM), Sonication is recommended. DMSO: 225.0 mg/mL (478.4 mM), Sonication is recommended. |
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL, Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 |
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