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JTT-654

CAT: 0804-HY-161449Size: 1 EachDry Ice: NoHazardous: No
CAT#:0804-HY-161449Size:1 Each
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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
[1]Heitaku S, et al. An 11-Beta Hydroxysteroid Dehydrogenase Type 1 Inhibitor, JTT-654 Ameliorates Insulin Resistance and Non-obese Type 2 Diabetes. Biol Pharm Bull. 2023;46 (7) :969-978.|[2]Heitaku S, et al. JTT-654, an 11-beta hydroxysteroid dehydrogenase type 1 inhibitor, improves hypertension and diabetic kidney injury by suppressing angiotensinogen production. J Pharmacol Sci. 2024 Apr;154 (4) :246-255.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2

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