BMS-986235

BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC 50 s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure In Vitro BMS-986235 (LAR-1219) inhibits neutrophil chemotaxis and stimulats macrophage phagocytosis, key end points to promote resolution of inflammation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . BMS-986235 (1 mg/kg; p.o.) treatment shows the C max , T 1/2 , AUC 0-inf , and bioavailability (BA) values of 160 nmol/L, 0.68 hours,120 nmol/L•h, and 24%, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6 mice 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) Dosage: 1 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The C max , T 1/2 , AUC 0-inf , and bioavailability (BA) values were 160 nmol/L, 0.68 hours, 120 nmol/L•h, and 24%, respectively. IC50& Target:EC50: 0.41 nM (human FPR2), 3.4 nM (mouse FPR2), 2800 nM (human FPR1)

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