[CAS NO. 376638-65-2] BVT-14225
PRODUCTS SPECIFICATIONS [376638-65-2]
DESCRIPTION [376638-65-2]
Overview
| MDL | MFCD25976913 |
|---|---|
| Molecular Weight | 401.93 |
| Molecular Formula | C16H20ClN3O3S2 |
| SMILES | O=C(N(CC)CC)CC1=CSC(NS(=O)(C2=CC=CC(Cl)=C2C)=O)=N1 |
1 Publications Citing Use of MCE
Summary
BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 ( 11β-HSD1 ) inhibitor with an IC 50 of 52 nM.
IC50 & Target
IC50: 52 nM (11β-HSD1) [1]
In Vitro
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 IC 50 for 11β-HSD1 on a human enzyme assay of 52 nM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 248.80 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [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.
- [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.
