2. GPCR/G Protein TGF-beta/Smad Stem Cell/Wnt Immunology/Inflammation
  3. Formyl Peptide Receptor (FPR) Arrestin PKA Interleukin Related
  4. 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.

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BMS-986331

BMS-986331 Chemical Structure

CAS No. : 2375684-52-7

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BMS-986331 Related Antibodies

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

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PKA PKAR PKACα

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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[1].

IC50 & Target[1]

Arrestin-2/β-Arrestin 1

 

Arrestin-3/β-Arrestin 2

 

IL-10

 

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC
Rat[1] 3 mg/kg p.o. 50 nM 200 nM·h
Rat[1] 300 mg/kg p.o. 22000 nM 25000 nM·h
In Vivo

BMS-986331 (Compound 16) (10 mg/kg; p.o.; single dose) induces a 105% increase in plasma IL-10 levels in LPS-challenged rats[1].
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.

Animal Model: Rats were subjected to permanent coronary artery occlusion to induce myocardial infarction (MI) and subsequent heart failure[1].
Dosage: 0.1, 1, 10 mg/kg/day
Administration: Oral administration; once daily; formulation: PEG 400/PG/TPGS/water (40:10:10:40); dosing initiated 48 h post-MI; for 6 weeks
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.
Animal Model: Rats[1].
Dosage: 3 mg/kg; 300 mg/kg (high dose)
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
Result: At 3 mg/kg, oral exposure was sufficient for efficacy.
No obvious toxic reactions observed.
Molecular Weight

535.88

Formula

C25H22ClF3N3O3P
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BMS-986331 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-9863312375684-52-7BMS986331BMS 986331Formyl Peptide Receptor (FPR)ArrestinPKAInterleukin RelatedProtein kinase AILGα12Gαi2β-arrestin1β-arrestin2Gα13GαoAheart failureIL-10N-Formyl Peptide Receptor 2FPR2Inhibitorinhibitorinhibit

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