BMS-986331 |
Katalog-Nr.GC79327
One-Click Copy Product Info
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BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC 50 of 0.5 nM in humans and 1 nM in rats.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2375684-52-7
Sample solution is provided at 25 µL, 10mM.
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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].
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].
References:
[1]. Shirude PS, et al. From Lead to Clinical Candidate: Discovery of BMS-986331 as a Potent and Selective N -Formyl Peptide Receptor 2 Agonist. J Med Chem. 2026;69(4):4078-4089.
| Cas No. | 2375684-52-7 | SDF | |
| Formula | C25H22ClF3N3O3P | M.Wt | 535.88 |
| Löslichkeit | DMSO: 4.17 mg/mL (7.78 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8661 mL | 9.3304 mL | 18.6609 mL |
| 5 mM | 373.2 μL | 1.8661 mL | 3.7322 mL |
| 10 mM | 186.6 μL | 933 μL | 1.8661 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)