BMS-986331
Based on 1 Customer Validation
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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- Purity : 99.81%
- CAS No.: 2375684-52-7
- 화학식: C25H22ClF3N3O3P
- 분자량:535.88
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All Arrestin Isoforms
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Biological Activity
제품 설명
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.
Parmacokinetics
In Vivo
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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Appearance Solid
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분자량 535.88
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화학식 C25H22ClF3N3O3P
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Color White to off-white
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 4.17 mg/mL (7.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8661 mL | 9.3304 mL | 18.6609 mL | 46.6522 mL |
| 5 mM | 0.3732 mL | 1.8661 mL | 3.7322 mL | 9.3304 mL |
BMS-986331 Related Classifications
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