2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. Protease-Activated Receptor-1 antagonist 2

Protease-Activated Receptor-1 antagonist 2 

目录号: HY-143314
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摩尔计算器

Protease-Activated Receptor-1 antagonist 2 是一种具有口服活性的选择性蛋白酶激活受体-1 (PAR-1) 拮抗剂，其 IC50 值为 7 nM。Protease-Activated Receptor-1 antagonist 2 具有良好的药代动力学特性，可用于心血管疾病 (CVD) 的相关研究，如动脉粥样硬化和再狭窄。

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Protease-Activated Receptor-1 antagonist 2 Chemical Structure

Protease-Activated Receptor-1 antagonist 2 Chemical Structure

CAS No. : 1454588-34-1

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Protease-Activated Receptor-1 antagonist 2 相关抗体

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生物活性

Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis[1].

IC50 & Target

IC50: 7 nM (PAR-1)[1].
体内研究
(In Vivo)

Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC50 of 7 nM[1].
Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC0−24 h and Cmax in a dose-dependent manner[1].
Protease-Activated Receptor-1 antagonist 2 doesn’t elicit any prominent liver bioactivation or tissue toxicity signals up to an AUC of 44 μM•h[1].

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

Animal Model: Rat, monkey, dog[1]
Dosage: i.v. (3 mpk for rat, 0.3 mpk for dog and monkey), p.o (10 mpk for rat, 1 mpk for dogs and monkey)
Administration: i.v., p.o (Pharmacokinetic Analysis)
Result: Pharmacokinetic parameters.
compound FLIPR IC50 (nM) MRT (R;c D; d Me) F% (R;f D; g Mh) predicted human MRT
Protease-Activated Receptor-1 antagonist 2 7 1.9; 18; 25 54; 100; 37 20−48
分子量

423.46

Formula

C24H23F2N3O2
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

Protease-Activated Receptor-1 antagonist 2 相关分类

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  • 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.

Keywords:

Protease-Activated Receptor-1 antagonist 21454588-34-1Protease Activated Receptor (PAR)Thrombin receptorsProtease-Activated Receptor-1PAR-1 AntagonistatherosclerosisrestenosisInhibitorinhibitorinhibit

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