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。

Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC 50 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].

Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC 50 of 7 nM [1]. Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC 0 24 h and C max 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]. 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 IC 50 (nM) ex vivo platelet agg % eff @ 1/0.3 mpk (t, h) hERG IC 50 (μM) Pgp (BA/AB) H; R; control P app b Hep Cl (μL/min/10 6 cells) R; D; M; H Cl (mL/min/kg) (R; c D; d M e ) CL U (mL/min/kg) (R; c D; d M e ) V d (L/kg) (R; c D; d M e ) V d,U (L/kg) (R; c D; d M e ) f U, plasma (L/kg) (R; D; M) MRT (R; c D; d M e ) F% (R; f D; g M h ) predicted human MRT Panlabs (Disc. Sci) Protease-Activated Receptor-1 antagonist 2 7 100 (24)/100 (24) >60 1.1; 2.6; 0.6 分子量 423.46 Formula C 24 H 23 F 2 N 3 O 2 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. 参考文献 [1]. Mihirbaran Mandal, et al. Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. J Med Chem. 2022 Apr 14;65(7):5575-5592. Data Sheet (488 KB) 半岛bd体育手机客户端 使用指南 (1538 KB) [1]. Mihirbaran Mandal, et al. Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery. J Med Chem. 2022 Apr 14;65(7):5575-5592. 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 * kg g mg μg ng pg = M mM μM nM pM × L mL μL × The dilution calculator equation Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C 1 V 1 = C 2 V 2 浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final) M mM μM nM pM × L mL μL = M mM μM nM pM × L mL μL C1 V1 C2 V2 Powered by Bioz See more details on Bioz Keywords: Protease-Activated Receptor-1 antagonist 2 1454588-34-1 Protease Activated Receptor (PAR) Thrombin receptors Protease-Activated Receptor-1 PAR-1 Antagonist atherosclerosis restenosis Inhibitor inhibitor inhibit 您最近查看的半岛bd体育手机客户端 :

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years