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首页-小分子抑制剂&激动剂-GPCR-Formyl peptide receptor (FPR)-BMS-986235
BMS-986235

Chemical Structure : BMS-986235

CAS No.: 2253947-47-4

BMS-986235 (LAR-1219, BMS986235, LAR1219)

货号: PC-49033Not For Human Use, Lab Use Only.

BMS-986235 (LAR-1219) is a potent, selective, and orally bioavailable agonist of formyl peptide receptor 2 (FPR2) with EC50 of 0.4 nM (hFPR2), >7,000-fold selectivity over FPR1.

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10 mg ¥2480 In stock
25 mg ¥4280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BMS-986235 (LAR-1219) is a potent, selective, and orally bioavailable agonist of formyl peptide receptor 2 (FPR2) with EC50 of 0.4 nM (hFPR2), >7,000-fold selectivity over FPR1.
BMS-986235 produced concentration-dependent modulation of BRET signals for Gαi1, Gαi2, Gαi3, GαoA, and GαoB biosensors following FPR2 activation (EC50=5-13 nM), 164- to 614-fold selectivity over FPR1 activation.
BMS-986235 improved mouse survival, reduced left ventricular area, reduced scar area, and preserved wall thickness, inhibited neutrophil chemotaxis and stimulated macrophage phagocytosis, key end points to promote resolution of inflammation.
BMS-986235 preserved viable myocardium, attenuated left ventricular remodeling, and increased ejection fraction in rats following MI.

物理化学性质&存储条件

分子量 361.349
分子式 C18H17F2N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-((3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl)-3-phenylurea

参考文献

1. Yoshikazu Asahina, et al. J Med Chem. 2020 Sep 10;63(17):9003-9019.

2. Ricardo A García, et al. JACC Basic Transl Sci. 2021 Aug 23;6(8):676-689.

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