BMS-963272
Based on 1 Customer Validation
BMS-963272 is an orally active and selective MGAT2 inhibitor (IC50 = 7.1 nM), used for the study of metabolic disorders and inflammatory diseases.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.02%
- CAS No.: 1441057-15-3
- Formule: C24H21F6N5O2
- Masse moléculaire:525.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
BMS-963272 (10 min) has good metabolic properties, with 100% metabolic stability in both human and mouse liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obese mouse model (C57BL/6J)[1]
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.), twice daily, for 24 days
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Result:Reduced body weight gain by 8.6%-14.3%; significantly decreased food intake by 18%-27%.
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Animal Model:CDAHFD-induced NASH mouse (C57BL/6J mice) model (CDAHFD: Choline-Deficient, Amino Acid-Defined High Fat Diet)[2]
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Dosage:0.3 mg/kg and 3.0 mg/kg
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Administration:Oral gavage (p.o.), once daily, for 8 weeks
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Result:Significantly reduced liver fibrosis, decreased ALT and AST levels, and reduced TNFa expression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1441057-15-3
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Appearance Solid
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Masse moléculaire 525.45
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Formule C24H21F6N5O2
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Color Off-white to light yellow
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SMILES
CC1=CC=C(C2=C(C(N[C@@](C3=CC=C(C=C3)OCCCC(F)(F)F)(C(F)(F)F)C2)=O)C4=NN=NN4)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 250 mg/mL (475.78 mM; Need ultrasonic; 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)
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: ≥ 2.08 mg/mL (3.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Turdi H, et al. Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders. J Med Chem. 2021 Oct 14;64(19):14773-14792. [Content Brief]
[2]. Cheng D, et al. MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity. Cell Metab. 2022 Nov 1;34(11):1732-1748.e5. [Content Brief]
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 |
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| DMSO | 1 mM | 1.9031 mL | 9.5157 mL | 19.0313 mL | 47.5783 mL |
| 5 mM | 0.3806 mL | 1.9031 mL | 3.8063 mL | 9.5157 mL | |
| 10 mM | 0.1903 mL | 0.9516 mL | 1.9031 mL | 4.7578 mL | |
| 15 mM | 0.1269 mL | 0.6344 mL | 1.2688 mL | 3.1719 mL | |
| 20 mM | 0.0952 mL | 0.4758 mL | 0.9516 mL | 2.3789 mL | |
| 25 mM | 0.0761 mL | 0.3806 mL | 0.7613 mL | 1.9031 mL | |
| 30 mM | 0.0634 mL | 0.3172 mL | 0.6344 mL | 1.5859 mL | |
| 40 mM | 0.0476 mL | 0.2379 mL | 0.4758 mL | 1.1895 mL | |
| 50 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9516 mL | |
| 60 mM | 0.0317 mL | 0.1586 mL | 0.3172 mL | 0.7930 mL | |
| 80 mM | 0.0238 mL | 0.1189 mL | 0.2379 mL | 0.5947 mL | |
| 100 mM | 0.0190 mL | 0.0952 mL | 0.1903 mL | 0.4758 mL |
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