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BMS-986235

BMS-986235(LAR-1219)是一种选择性、具有口服活性的甲酰肽受体2(FPR2)激动剂,对hFPR2和mFPR2的EC50分别为0.41nM和3.4nM。BMS-986235具有预防心力衰竭的潜力。

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BMS-986235的二维码
  • 库存: 现货
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  • 5mg
    ¥4850.00
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    ¥8412.00
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  • 50mg
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  • 货号: ajcx30288
  • CAS: 2253947-47-4
  • 别名: LAR-1219
  • 分子式: C18H17F2N3O3
  • 分子量: 361.34
  • 纯度: >98%
  • 溶解度:
  • 储存: Store at -20°C
  • 库存: 现货

Background

BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure[1].


BMS-986235 (LAR-1219) inhibits neutrophil chemotaxis and stimulats macrophage phagocytosis, key end points to promote resolution of inflammation[1].


BMS-986235 (LAR-1219) (0.3 mg/kg; p.o.; daily for 24 days) can attenuate left ventricle and global cardiac remodeling after left anterior descending (LAD) in mice[1].BMS-986235 (1 mg/kg; p.o.) treatment shows the Cmax, T1/2, AUC0-inf, and bioavailability (BA) values of 160 nmol/L, 0.68 hours,120 nmol/L?h, and 24%, respectively[1]. Animal Model: Male C57BL/6 mice[1]


[1]. Asahina Y, et al. Discovery of BMS-986235/LAR-1219: A Potent Formyl Peptide Receptor 2 (FPR2) Selective Agonist for the Prevention of Heart Failure [published online ahead of print, 2020 May 24]. J Med Chem. 2020;10.1021/acs.jmedchem.9b02101.

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