JTT-654
JTT-654 is an orally active, potent and selective11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. The IC50 of JTT-654 for 11β-HSD1 is 4.65, 0.97, and 0.74 nM in human, rat, and mouse recombinant enzymes, respectively. JTT-654 showed competitive inhibition against human recombinant enzyme. The IC50 value for human 11β-HSD2 is > 30 μM (human 11β-HSD2 is responsible for the reverse reaction against human 11β-HSD1) . JTT-654 ameliorates insulin resistance and non-obese type 2 diabetes by inhibiting adipose tissue and liver 11β-HSD1[1][2].
Product Specifications
CAS Number
916828-66-5
UNSPSC
12352005
Target
11β-HSD
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/jtt-654.html
Solubility
10 mM in DMSO
Smiles
FC(F)(F)C1=CC=CC=C1[C@H]2CN(C(C3=C(C4CC4)N(C5CCN(C(C6(CC6)CO)=O)CC5)N=C3)=O)CC2
Molecular Formula
C28H33F3N4O3
Molecular Weight
530.58
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Frequently Asked Questions
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