BMS-986235
Based on 1 publication(s) in Google Scholar
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.
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- Reinheit: 99.84%
- CAS. Nr.: 2253947-47-4
- Formel: C18H17F2N3O3
- Molecular Weight:361.34
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) BMS-986235
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Biologische Aktivität
EC50: 0.41 nM (human FPR2), 3.4 nM (mouse FPR2), 2800 nM (human FPR1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
57 nM
Compound: 98; BMS-986235
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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
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[PMID: 33486199] |
| Peritoneal macrophage | EC50 |
<1 nM
Compound: 1
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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
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[PMID: 35707160] |
| Peritoneal macrophage | EC50 |
2 nM
Compound: 98; BMS-986235
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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
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[PMID: 33486199] |
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.
? BMS-986235 (1 mg/kg; p.o.) treatment shows the Cmax, T1/2, AUC0-inf, and bioavailability (BA) values of 160 nmol/L, 0.68 hours,120 nmol/L?h, and 24%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice[1]
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Dosage:0.3 mg/kg
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Administration:P.o.; daily for 24 days
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Result:Left ventricle (LV) chamber remodeling is attenuated after myocardial infarction (MI). Reduced infarct length by 39% relative to vehicle.
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Animal Model:Male mice (BALB/cCrSlc)[1]
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Dosage:1 mg/kg
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Administration:P.o. (Pharmacokinetic Analysis)
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Result:The Cmax, T1/2, AUC0-inf, and bioavailability (BA) values were 160 nmol/L, 0.68 hours, 120 nmol/L•h, and 24%, respectively.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2253947-47-4
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Appearance Solid
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Molecular Weight 361.34
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Formel C18H17F2N3O3
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Color White to off-white
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SMILES
O=C(NC1=CC=CC=C1)N[C@@H]2C(NC[C@H]2C3=C(F)C=C(OC)C=C3F)=O
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Synonyms
LAR-1219
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Failure to Resolve Inflammation Contributes to Juvenile-Onset Cardiomyopathy in a Mouse Model of Duchenne Muscular Dystrophy. [Abstract]2024 Aug 15:2024.08.15.607998. PMID: 39185176
Lösungsmittel & Löslichkeit
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.
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7675 mL | 13.8374 mL | 27.6748 mL | 69.1869 mL |
| 5 mM | 0.5535 mL | 2.7675 mL | 5.5350 mL | 13.8374 mL | |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7675 mL | 6.9187 mL | |
| 15 mM | 0.1845 mL | 0.9225 mL | 1.8450 mL | 4.6125 mL | |
| 20 mM | 0.1384 mL | 0.6919 mL | 1.3837 mL | 3.4593 mL | |
| 25 mM | 0.1107 mL | 0.5535 mL | 1.1070 mL | 2.7675 mL | |
| 30 mM | 0.0922 mL | 0.4612 mL | 0.9225 mL | 2.3062 mL | |
| 40 mM | 0.0692 mL | 0.3459 mL | 0.6919 mL | 1.7297 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5535 mL | 1.3837 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4612 mL | 1.1531 mL | |
| 80 mM | 0.0346 mL | 0.1730 mL | 0.3459 mL | 0.8648 mL | |
| 100 mM | 0.0277 mL | 0.1384 mL | 0.2767 mL | 0.6919 mL |
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