Product 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].
Formula: C28H33F3N4O3
References: [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.
CAS Number: 916828-66-5
Molecular Weight: 530.58
Research Area: Metabolic Disease
Solubility: 10 mM in DMSO
Target: 11β-HSD