| Bioactivity | 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]. |
| Target | IC50: 4.65 ± 0.28 nM (human 11β-HSD1), 0.97 ± 0.019 nM (rat 11β-HSD1), 0.74 ± 0.050 nM (rat 11β-HSD1), > 30 μM (human 11β-HSD2) |
| Invitro | JTT-654（0.1-10 μM，24 h）对可的松 (HY-17461) 处理的 3T3-L1 脂肪细胞中血管紧张素原的产生具有抑制作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> JTT-654 相关抗体: |
| In Vivo | JTT-654（1-10 mg/kg，口服，单次）对肝脏和脂肪组织 11β-HSD1 活性有抑制作用[1]。JTT-654（1-10 mg/kg，口服，每天一次，持续 4 d）显着减弱可的松 (HY-17461) 在大鼠中的作用[1]。JTT-654（1.5-15 mg/kg，口服，每天两次，持续 19 d）可改善非肥胖 2 型糖尿病大鼠模型的胰岛素抵抗和高血糖[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| CAS | 916828-66-5 |
| Formula | C28H33F3N4O3 |
| Molar Mass | 530.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |