1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. PF-06815345

PF-06815345 是一种具有口服活性且有效的前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 抑制剂,IC50 为 13.4 μM。 PF-06815345 显着降低小鼠体内的 PCSK9 水平。

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PF-06815345 Chemical Structure

PF-06815345 Chemical Structure

CAS No. : 1900686-46-5

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PF-06815345 的其他形式现货产品:

Customer Review

Other Forms of PF-06815345:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-06815345 is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 significantly decreases the PCSK9 level in vivo in mouse[1][2].

IC50 & Target

IC50: >20 μM (cell based), 13.4 (cell free) for Proprotein convertase subtilisin/kexin type 9 (PCSK9)[2]

体外研究
(In Vitro)

PF-06815345(实施例 7)(1-30 μM;5-1440 分钟)在人肠细胞和肝细胞中的 CLint 值分别为 <82.9 μL/min/mg 和 97.6 μL/min/mg[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

PF-06815345(实施例 7)(100-500 mg/kg;口服;单剂量)降低人源化 PCSK9 小鼠模型中的 PCSK9 水平。处理 4 小时后,以 500 mg/kg 的剂量将血浆 PCSK9 降低了 72%[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

598.03

Formula

C27H29ClFN9O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

PF-06815345 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PF-06815345
目录号:
HY-112598
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