BMS-986172
Based on 1 Customer Validation
BMS-986172 is an orally active and selective Monoacylglycerol acyltransferase 2 (MGAT2) inhibitor with an IC50 of 4.6 nM and 20 nM for hMGAT2 and mMGAT2, respectively. BMS-986172 reduces food intake and body weight. BMS-986172 can be used for the researches of metabolic diseases, such as obesity .
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.48%
- No. CAS: 1808258-99-2
- Fòrmula: C24H22F7N7O3
- Peso molecular:589.47
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Almacenamiento:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
hMGAT2 4.6 nM (IC50) |
mMGAT2 20 nM (IC50) |
hMGAT3 16 μM (IC50) |
In Vitro
In Vivo
BMS-986172 (3 mg/kg, p.o., once a day for 4 days) does not change body weight in MGAT2 knockout mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Diet-induced obesity (DIO) mice models[1]
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Dosage:0.01, .03, 0.1, 0.3 and 1 mg/kg
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Administration:Orally administration, once a day for 21 days
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Result:Reduced 24 h food intake (21 to 34%).
Reduced body weight at doses of 0.1 mg/kg and above with 11.6, 6.1, and 8.9% reductions at 0.1, 0.3, and 1.0 mg/kg doses, respectively.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1808258-99-2
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Appearance Solid
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Peso molecular 589.47
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Fòrmula C24H22F7N7O3
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Color White to off-white
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SMILES
FC1=C([C@]2(C(F)(F)F)CC(C3=NN(C=C3)CC4CC4)=C(C(N2)=O)N5N=NNC5=O)C=CC(OCCCC(F)(F)F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (169.64 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Protocolo
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
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 (protect from light, stored under nitrogen). 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 | 1.6964 mL | 8.4822 mL | 16.9644 mL | 42.4110 mL |
| 5 mM | 0.3393 mL | 1.6964 mL | 3.3929 mL | 8.4822 mL | |
| 10 mM | 0.1696 mL | 0.8482 mL | 1.6964 mL | 4.2411 mL | |
| 15 mM | 0.1131 mL | 0.5655 mL | 1.1310 mL | 2.8274 mL | |
| 20 mM | 0.0848 mL | 0.4241 mL | 0.8482 mL | 2.1205 mL | |
| 25 mM | 0.0679 mL | 0.3393 mL | 0.6786 mL | 1.6964 mL | |
| 30 mM | 0.0565 mL | 0.2827 mL | 0.5655 mL | 1.4137 mL | |
| 40 mM | 0.0424 mL | 0.2121 mL | 0.4241 mL | 1.0603 mL | |
| 50 mM | 0.0339 mL | 0.1696 mL | 0.3393 mL | 0.8482 mL | |
| 60 mM | 0.0283 mL | 0.1414 mL | 0.2827 mL | 0.7068 mL | |
| 80 mM | 0.0212 mL | 0.1060 mL | 0.2121 mL | 0.5301 mL | |
| 100 mM | 0.0170 mL | 0.0848 mL | 0.1696 mL | 0.4241 mL |
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