BMS-820132
Based on 1 Customer Validation
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.75%
- No. CAS: 1001419-18-6
- Fòrmula: C26H33N6O7P
- Peso molecular:572.55
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Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
BMS-820132 (10-200 mg/kg; po; once daily for 1 mo) results in body weight reduction in normal rat but not ZDF rats, indicating that the toxicity is secondary to the exaggerated pharmacology of potent GK activation[2].
BMS-820132 (10 mg/kg, 60 mg/kg, 120 mg/kg; po; once daily for 1 mo) results insignificant effects on dogs food consumption[2].
Pharmacokinetic Analysis in Animal Model[1]
| Route | Dose (mg/kg) | Cmax (μM) | Tmax (h) | AUC0-24 h (μM·h) | T1/2 (h) | CLTp (mL/min/kg) | Vss (L/kg) | F (L/kg) | |
| mouse | iv | 2.5 | 24.9 | 2.1 | 2.9 | 0.3 | |||
| po | 5 | 14.1 | 0.5 | 49.7 | 100 | ||||
| rat | iv | 2.5 | 16.6 | 0.9 | 4.4 | 0.3 | |||
| po | 5 | 13.0 | 0.9 | 29.5 | 90 | ||||
| dog | iv | 3 | 12.3 | 1.8 | 7.2 | 0.5 | |||
| po | 3 | 4.9 | 0.8 | 8.0 | 66 | ||||
| monkey | iv | 3 | 3.8 | 1.9 | 22.7 | 1.1 | |||
| po | 3 | 3.8 | 1.3 | 0.57 | 15 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zucker diabetic fatty (ZDF) rats and normal SD rats[2]
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Dosage:10 mg/kg, 50 mg/kg, 200 mg/kg
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Administration:PO; once daily for 1 month
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Result:Resulted reductions in body weight gains starting on day 7 in SD rats (11% lower than controls), but not ZDF rats.
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Animal Model:Beagle dogs[2]
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Dosage:10 mg/kg, 60 mg/kg, 120 mg/kg
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Administration:PO; once daily for 1 month
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Result:There were no meaningful differences in food consumption in dogs model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1001419-18-6
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Appearance Solid
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Peso molecular 572.55
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Fòrmula C26H33N6O7P
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Color White to off-white
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SMILES
O=C(NC1=NN(CP(OCC)(OCC)=O)C=C1)C2=CC(OC(C)C)=CC(OC3=NC=C(C(N4CCC4)=O)N=C3)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvente y solubilidad
DMSO : 25 mg/mL (43.66 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.37 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture and light)
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.
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)
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- 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 (sealed storage, away from moisture and light). 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 | 1.7466 mL | 8.7329 mL | 17.4657 mL | 43.6643 mL |
| 5 mM | 0.3493 mL | 1.7466 mL | 3.4931 mL | 8.7329 mL | |
| 10 mM | 0.1747 mL | 0.8733 mL | 1.7466 mL | 4.3664 mL | |
| 15 mM | 0.1164 mL | 0.5822 mL | 1.1644 mL | 2.9110 mL | |
| 20 mM | 0.0873 mL | 0.4366 mL | 0.8733 mL | 2.1832 mL | |
| 25 mM | 0.0699 mL | 0.3493 mL | 0.6986 mL | 1.7466 mL | |
| 30 mM | 0.0582 mL | 0.2911 mL | 0.5822 mL | 1.4555 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4366 mL | 1.0916 mL |
BMS-820132 Related Classifications
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