BMS-986235 [2253947-47-4]

Cat# HY-131180-5mg

Size : 5mg

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

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].

IC50 & Target

EC50: 0.41 nM (human FPR2), 3.4 nM (mouse FPR2), 2800 nM (human FPR1)[1]

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
57 nM
Compound: 98; BMS-986235
Inhibition of cell migration in human HL-60 cells incubated for 135 mins by transwell assay
Inhibition of cell migration in human HL-60 cells incubated for 135 mins by transwell assay
[PMID: 33486199]
Peritoneal macrophage EC50
<1 nM
Compound: 1
Induction of phagocytosis in mouse peritoneal macrophages assessed as increase in FITC signal preincubated with compound for 15 mins followed by zymosan addition and measured after 1 hr by Trypan Blue based FITC analysis
Induction of phagocytosis in mouse peritoneal macrophages assessed as increase in FITC signal preincubated with compound for 15 mins followed by zymosan addition and measured after 1 hr by Trypan Blue based FITC analysis
[PMID: 35707160]
Peritoneal macrophage EC50
2 nM
Compound: 98; BMS-986235
Induction of phagocytosis in C57BL6 mouse peritoneal macrophages assessed as increase in FITC signal preincubated with compound for 15 mins followed by zymosan addition and measured after 90 mins by Trypan Blue based FITC analysis
Induction of phagocytosis in C57BL6 mouse peritoneal macrophages assessed as increase in FITC signal preincubated with compound for 15 mins followed by zymosan addition and measured after 90 mins by Trypan Blue based FITC analysis
[PMID: 33486199]
In Vitro

BMS-986235 (LAR-1219) inhibits neutrophil chemotaxis and stimulats macrophage phagocytosis, key end points to promote resolution of inflammation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (276.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7675 mL 13.8374 mL 27.6748 mL
5 mM 0.5535 mL 2.7675 mL 5.5350 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 2.5 mg/mL (6.92 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation
References

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