BMS-986331
BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC50 of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure.
For research use only. We do not sell to patients.
- CAS No.: 2375684-52-7
- Formula: C25H22ClF3N3O3P
- Molecular Weight:535.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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All Arrestin Isoforms
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Biological Activity
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Arrestin-2/β-Arrestin 1 |
Arrestin-3/β-Arrestin 2 |
IL-10 |
BMS-986331 (Compound 16) potently activates human FPR2 (hFPR2) with an EC50 of 0.5 nM and exhibits 500-fold selectivity over hFPR1; it also activates rat FPR2 with an EC50 of 0.6 nM and 280-fold selectivity over rat FPR1[1].
BMS-986331 shows high chemical stability at pH 1, with a half-life > 500 min[1].
BMS-986331 (100 nM) induces a 211% increase in IL-10 levels in human whole blood[1].
BMS-986331 potently activates multiple signaling pathways via human FPR2 in HEK293 cells, with EC50 values of 0.50 nM for Gαi2, 0.56 nM for GαoA, 16 nM for Gα12/P115, and 40 nM for Gα13/PDZ-RhoGEF[1].
BMS-986331 induces the recruitment of β-arrestin1 and β-arrestin2 to human FPR2 in HEK293 cells, with EC50 values of 46 nM for β-arrestin1 and 19 nM for β-arrestin2[1].
BMS-986331 inhibits OATP1B3 with an IC50 of 12 μM[1].
BMS-986331 retains 88% of its concentration in human liver microsomes and 33% in rat liver microsomes after incubation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BMS-986331 (0.1-10 mg/kg/day; p.o.; once daily; 6 weeks) preserves infarct wall thickness and improves left ventricular ejection fraction in rats with permanent coronary artery occlusion[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats were subjected to permanent coronary artery occlusion to induce myocardial infarction (MI) and subsequent heart failure[1].
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Dosage:0.1, 1, 10 mg/kg/day
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Administration:Oral administration; once daily; formulation: PEG 400/PG/TPGS/water (40:10:10:40); dosing initiated 48 h post-MI; for 6 weeks
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Result:At 1 mg/kg and 10 mg/kg doses, significantly preserved infarct wall thickness.
Achieved 9% absolute increase in left ventricular ejection fraction relative to vehicle.
Picrosirius red staining of left ventricular histological cross sections revealed improved myocardial structure.
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Animal Model:Rats[1].
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Dosage:3 mg/kg; 300 mg/kg (high dose)
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Administration:Oral administration; 3 mg/kg with formulation: 10% EtOH, 70% PEG 400, 10% TPGS, 10% water; 300 mg/kg with spray dried dispersion (SDD) suspension (25% API in HPMCAS); 2-week toxicity study with 300 mg/kg/day
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Result:At 3 mg/kg, oral exposure was sufficient for efficacy.
No obvious toxic reactions observed.
Chemical Information
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CAS No. 2375684-52-7
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Molecular Weight 535.88
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Formula C25H22ClF3N3O3P
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SMILES
CP(C(C=CC=C1)=C1C(C(F)=C2F)=CC=C2N(CC3)C([C@@H]3NC(NC4=CC=C(Cl)C=C4F)=O)=O)(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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