BMS-986235

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].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

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] Dosage: 0.3 mg/kg Administration: P.o.; daily for 24 days Result: Left ventricle (LV) chamber remodeling is attenuated after myocardial infarction (MI). Reduced infarct length by 39% relative to vehicle. Animal Model: Male mice (BALB/cCrSlc)[1] Dosage: 1 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The Cmax, T1/2, AUC0-inf, and bioavailability (BA) values were 160 nmol/L, 0.68 hours, 120 nmol/L•h, and 24%, respectively.

[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.