| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1). BVT-14225 is a selective 11β-HSD1 inhibitor with an IC50 of 52 nM. It displays >200-fold selectivity over human and murine 11β-HSD2. The compound inhibits the conversion of inert cortisone into active cortisol.
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| ln Vitro |
In hyperglycemic mice, selective inhibition of 11β-HSD1 lowers blood glucose levels. Selective inhibitors of 11β-HSD1 exhibit significant promise in the treatment of numerous untreated medical conditions, including obesity, type 2 diabetes, and metabolic syndrome (a complex disorder). In enzymatic tests, BVT-14225 exhibited strong activity, exhibiting 90% inhibition at 10 μM. In a human enzyme assay, its IC50 for 11β-HSD1 is 52 nM [2].
BVT-14225 selectively inhibits 11β-HSD1 with an IC50 of 52 nM. In enzymatic tests, it shows high activity with 90% inhibition at 10 μM. The compound displays >200-fold selectivity over human and murine 11β-HSD2. Selective inhibitors of 11β-HSD1 exhibit significant promise in the treatment of numerous conditions, including obesity, type 2 diabetes, and metabolic syndrome. |
| ln Vivo |
In vivo, BVT-14225 has been studied for its ability to inhibit 11β-HSD1 and modulate glucocorticoid metabolism. Selective inhibitors of 11β-HSD1 exhibit significant promise in the treatment of numerous medical conditions, including obesity, type 2 diabetes, and metabolic syndrome. Further in vivo studies are needed to fully characterize its therapeutic potential.
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| Enzyme Assay |
In vitro enzyme assays for BVT-14225 involve measuring its inhibition of 11β-HSD1 activity. 11β-HSD1 is incubated with its substrate, cortisone, and various concentrations of BVT-14225. The conversion of cortisone to cortisol is measured by HPLC, mass spectrometry, or immunoassay. IC50 values (52 nM) are determined from concentration-response curves.
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| Cell Assay |
In vitro cellular assays for BVT-14225 involve treating cells expressing 11β-HSD1 with the compound and measuring cortisol production. Cells are treated with various concentrations of BVT-14225 and incubated with cortisone. Cortisol levels in the culture medium are measured by ELISA or mass spectrometry. The compound's ability to inhibit 11β-HSD1 in cellular contexts is demonstrated.
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| Animal Protocol |
In vivo animal studies for BVT-14225 typically involve administration to rodent models of metabolic syndrome, obesity, or diabetes. Efficacy is assessed by measuring cortisol levels, glucose tolerance, insulin sensitivity, and body weight. Selective 11β-HSD1 inhibitors have shown promise in treating obesity and type 2 diabetes.
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| ADME/Pharmacokinetics |
BVT-14225 has a molecular weight of 387.90 and a molecular formula of C15H18ClN3O3S2. It is a selective 11β-HSD1 inhibitor with an IC50 of 52 nM. The compound is widely used as a reference tool for studying 11β-HSD1-mediated processes. Further pharmacokinetic studies are needed to fully characterize its profile.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of BVT-14225 are limited. The compound is a selective 11β-HSD1 inhibitor that displays >200-fold selectivity over 11β-HSD2. This selectivity may contribute to a favorable safety profile. Comprehensive toxicological evaluation is needed before clinical development. The compound should be handled with appropriate safety precautions.
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| References |
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| Additional Infomation |
BVT-14225 is a selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with an IC50 of 52 nM. It displays >200-fold selectivity over human and murine 11β-HSD2. BVT-14225 inhibits the conversion of inert cortisone into active cortisol and shows high activity in enzymatic tests. It is widely used as a reference tool for studying 11β-HSD1-mediated processes and has potential applications in obesity, type 2 diabetes, and metabolic syndrome.
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| Molecular Formula |
C16H20N3O3S2CL
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| Molecular Weight |
401.9313
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| Exact Mass |
401.063
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| CAS # |
376638-65-2
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| PubChem CID |
6918663
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| Appearance |
White to off-white solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
551
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| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
PNFMZAHWOASGJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H20ClN3O3S2/c1-4-20(5-2)15(21)9-12-10-24-16(18-12)19-25(22,23)14-8-6-7-13(17)11(14)3/h6-8,10H,4-5,9H2,1-3H3,(H,18,19)
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| Chemical Name |
2-[2-[(3-chloro-2-methylphenyl)sulfonylamino]-1,3-thiazol-4-yl]-N,N-diethylacetamide
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| Synonyms |
BVT14225 BVT 14225 BVT-14225
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~248.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4880 mL | 12.4400 mL | 24.8800 mL | |
| 5 mM | 0.4976 mL | 2.4880 mL | 4.9760 mL | |
| 10 mM | 0.2488 mL | 1.2440 mL | 2.4880 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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