BVT-14225
Based on 1 publication(s) in Google Scholar
BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 52 nM.
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- Pureté: 98.23%
- CAS No.: 376638-65-2
- Formule: C16H20ClN3O3S2
- Masse moléculaire:401.93
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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
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Publications Citing Use of MedChemExpress (MCE) BVT-14225
More
Activité biologique
IC50: 52 nM (11β-HSD1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
>200 μM
Compound: BVT-14225
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Inhibition of human 11beta-HSD2 expressed in CHO cells
Inhibition of human 11beta-HSD2 expressed in CHO cells
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[PMID: 17490884] |
| CHO | IC50 |
1.5 μM
Compound: BVT-14225
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Inhibition of human 11beta-HSD1 expressed in CHO cells
Inhibition of human 11beta-HSD1 expressed in CHO cells
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[PMID: 17490884] |
| HEK293 | IC50 |
0.0284 μM
Compound: BVT-14225
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Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay
Inhibition of human 11beta HSD1 expressed in HEK293 cells assessed as assessed as inhibition of [1,2-(n)3H]cortisone to [3H]-cortisol after 60 mins by scintillation proximity assay
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[PMID: 21873057] |
| Sf9 | IC50 |
52 nM
Compound: 1, BVT-14225
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Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay
Displacement of [3H]cortisone from human 11beta-HSD1 expressed in baculovirus-infected Sf9 cells after 1 hr by scintillation proximity assay
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[PMID: 20149650] |
Selective inhibition of 11β-HSD1 decreases blood glucose concentrations in hyperglycaemic mice. Selective inhibitors of 11β-HSD1 have considerable potential as treatments for a number of diseases of great unmet medical need such as type 2 diabetes, obesity and metabolic syndrome, a multifactorial disorder. BVT-14225 shows high activity in the enzyme assay with 90% inhibition at 10 μM. It has an IC50 for 11β-HSD1 on a human enzyme assay of 52 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 376638-65-2
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Appearance Solid
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Masse moléculaire 401.93
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Formule C16H20ClN3O3S2
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Color White to off-white
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SMILES
O=C(N(CC)CC)CC1=CSC(NS(=O)(C2=CC=CC(Cl)=C2C)=O)=N1
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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 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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Endocrinology
Conversion of Classical and 11-Oxygenated Androgens by Insulin-Induced AKR1C3 in a Model of Human PCOS Adipocytes. [Abstract]2022 Jul 1;163(7):bqac068. PMID: 35560164
Solvant et solubilité
DMSO : ≥ 100 mg/mL (248.80 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.
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: ≥ 2.5 mg/mL (6.22 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.22 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.
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 (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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Barf T, et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem. 2002 Aug 29;45(18):3813-5. [Content Brief]
[2]. Vicker N, et al. Novel non-steroidal inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1. J Steroid Biochem Mol Biol. 2007 May;104(3-5):123-9. [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, 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 | 2.4880 mL | 12.4400 mL | 24.8800 mL | 62.1999 mL |
| 5 mM | 0.4976 mL | 2.4880 mL | 4.9760 mL | 12.4400 mL | |
| 10 mM | 0.2488 mL | 1.2440 mL | 2.4880 mL | 6.2200 mL | |
| 15 mM | 0.1659 mL | 0.8293 mL | 1.6587 mL | 4.1467 mL | |
| 20 mM | 0.1244 mL | 0.6220 mL | 1.2440 mL | 3.1100 mL | |
| 25 mM | 0.0995 mL | 0.4976 mL | 0.9952 mL | 2.4880 mL | |
| 30 mM | 0.0829 mL | 0.4147 mL | 0.8293 mL | 2.0733 mL | |
| 40 mM | 0.0622 mL | 0.3110 mL | 0.6220 mL | 1.5550 mL | |
| 50 mM | 0.0498 mL | 0.2488 mL | 0.4976 mL | 1.2440 mL | |
| 60 mM | 0.0415 mL | 0.2073 mL | 0.4147 mL | 1.0367 mL | |
| 80 mM | 0.0311 mL | 0.1555 mL | 0.3110 mL | 0.7775 mL | |
| 100 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6220 mL |
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