1. Metabolic Enzyme/Protease
  2. 11β-HSD
  3. 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.

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JTT-654 Chemical Structure

JTT-654 Chemical Structure

CAS No. : 916828-66-5

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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].

IC50 & 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)[1]

In Vitro

JTT-654 (0.1-10 μM, 24 h) shows inhibitory effects on angiotensinogen production in Cortisone (HY-17461)-treated 3T3-L1 adipocytes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JTT-654 (1-10 mg/kg, Orally, single) shows inhibitory effect on liver and adipose tissue 11β-HSD1 activity[1].
JTT-654 (1-10 mg/kg, Orally, once daily for 4 d) significantly attenuates the effect of Cortisone (HY-17461) in Rats[1].
JTT-654 (1.5-15 mg/kg, Orally, twice daily, for 19 d) ameliorates insulin resistance and hyperglycemia in a non-obese type 2 diabetes rat model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rats (8 weeks old)[1]
Dosage: 1, 3, or 10 mg/kg
Administration: Orally, single administration
Result: The inhibitory effect for cortisone-cortisol conversion in liver and fat was dose dependent. In the 10 mg/kg JTT-654 group, the % inhibition in both tissues (Liver and Adipose) was almost 100% up to 8 h post-dose, and approximately 70% inhibition was still observed even at 24 h post-dose.
Animal Model: Male Wistar rats (7-week-old)[1]
Dosage: 1, 3, 10 mg/kg
Administration: Orally, once daily for 4 d, Cortisone was administered 1 h after JTT-654 administration on each day of dosing.
Result: Significantly attenuated the increase in fasted plasma glucose and insulin levels in a dose-dependent manner.
Animal Model: Non-obese type 2 diabetic Goto-Kakizaki (GK) Rats (8-week-old, male)[1]
Dosage: 1.5, 5, 15 mg/kg
Administration: Orally, twice daily, for 19 d
Result: Significantly reduced fasting plasma glucose and insulin levels, enhanced insulin-stimulated glucose oxidation in adipose tissue, and suppressed hepatic gluconeogenesis.
Molecular Weight

530.58

Formula

C28H33F3N4O3

CAS No.
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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JTT-654
Cat. No.:
HY-161449
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