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Protease-Activated Receptor-1 antagonist 2
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Protease-Activated Receptor-1 antagonist 2图片
CAS NO:1454588-34-1
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

Protease-Activated Receptor-1 antagonist 2 is an orally activeprotease-activated receptor-1(PAR-1) antagonist, with anIC50value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research ofcardiovascular 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 IC50of 7 nM[1].
Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC0–24 hand Cmaxin 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 μMoh[1].

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.
compoundFLIPR IC50(nM)MRT (R;cD;dMe)F% (R;fD;gMh)predicted human MRT
Protease-Activated Receptor-1 antagonist 271.9; 18; 2554; 100; 3720–48
分子量

423.46

Formula

C24H23F2N3O2

CAS 号

1454588-34-1

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.