BMS-986235是一种口服活性甲酰肽受体2 (FPR2) 激动剂,对人和小鼠FPR2的EC50分别为0.41 nM和3.4 nM。该化合物具有潜力用于心力衰竭的预防性研究。
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描述 | BMS-986235 (LAR-1219) is an orally active, selective agonist of formyl peptide receptor 2 (FPR2), with EC50 values of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 demonstrates promise for heart failure prevention[1]. |
体内研究 | BMS-986235 (LAR-1219) (0.3 mg/kg; pO.; daily for 24 days) exhibits the ability to mitigate left ventricular and overall cardiac remodeling following left anterior descending (LAD) coronary artery occlusion in mice[1]. BMS-986235 Treatment (1 mg/kg; oral administration) demonstrates maximum plasma concentration (Cmax), half-life (T1/2), area under the curve from time zero to infinity (AUC0-inf), and bioavailability (BA) values of 160 nmol/L, 0.68 hours, 120 nmol/L•h, and 24%, respectively[1]. |
体外研究 | BMS-986235 (LAR-1219) suppresses neutrophil chemotaxis and enhances macrophage phagocytosis, pivotal processes for facilitating inflammation resolution[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.77mL 0.55mL 0.28mL |
13.84mL 2.77mL 1.38mL |
27.67mL 5.53mL 2.77mL |
CAS号 | 2253947-47-4 |
分子式 | C18H17F2N3O3 |
分子量 | 361.343 |
别名 | LAR-1219 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 105 mg/mL(290.58 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |