An 11β-HSD1 inhibitor
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BVT 14225

Item No. 41224

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(3-chloro-2-methylphenyl)sulfonyl]amino]-N,N-diethyl-4-thiazoleacetamide
CAS Number
376638-65-2
Molecular Formula
C16H20ClN3O3S2
Formula Weight
401.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
ClC1=C(C)C(S(NC2=NC(CC(N(CC)CC)=O)=CS2)(=O)=O)=CC=C1
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)
InChi Key
PNFMZAHWOASGJC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $165

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    25 mg

    $275

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    Product Description

    BVT 14225 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1; IC50s = 52 and 284 nM for the human and mouse enzymes, respectively).1 It is selective for human 11β-HSD1 over human 11β-HSD2 (IC50 = >10,000 nM). It inhibits 11β-HSD1 by 55% in HEK293 cells expressing human HSD11B1, the gene encoding 11β-HSD1, when used at a concentration of 10 µM.2 BVT 14225 (50 mg/kg) reduces blood glucose levels in a rat model of diabetes induced by streptozotocin (Item No. 13104) and nicotinamide (Item No. 11127).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barf, T., Vallgårda, J., Emond, R., et al. Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1. J. Med. Chem. 45(18), 3813-3815 (2002).

    2. Navarrete-Vázquez, G., Morales-Vilchis, M.G., Estrada-Soto, S., et al. Synthesis of 2-{2-[(α/β-naphthalen-1-ylsulfonyl)amino]-1,3-thiazol-4-yl} acetamides with 11β-hydroxysteroid dehydrogenase inhibition and in combo antidiabetic activities. Eur. J. Med. Chem. 74, 179-186 (2014).