| Identification | Back Directory | [Name]
Urea, N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxo-3-pyrrolidinyl]-N'-phenyl- | [CAS]
2253947-47-4 | [Synonyms]
LAR-1219
BMS-986235
1-((3S,4R)-4-(2,6-Difluoro-4-methoxyphenyl)-2-oxopyrrolidin-3-yl)-3-phenylurea
Urea, N-[(3S,4R)-4-(2,6-difluoro-4-methoxyphenyl)-2-oxo-3-pyrrolidinyl]-N'-phenyl-
Inhibitor,BMS 986235,macrophage,phagocytosis,LAR 1219,heart,BMS986235,chemotaxis,failure,inhibit,LAR1219,inflammation,neutrophil | [Molecular Formula]
C18H17F2N3O3 | [MOL File]
2253947-47-4.mol | [Molecular Weight]
361.34 |
| Chemical Properties | Back Directory | [Boiling point ]
499.4±45.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
10.24±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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[1].
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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.
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| 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.
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| [References]
[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. DOI:10.1021/acs.jmedchem.9b02101 |
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