2. Metabolic Enzyme/Protease
  3. 11β-HSD
  4. JTT-654

JTT-654 是一种口服有效的选择性11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂。在人、大鼠和小鼠重组酶中，JTT-654 对 11β-HSD1 的 IC50 分别为 4.65、0.97 和 0.74 nM。 JTT-654 对人重组酶表现出竞争性抑制。JTT-654 对人 11β-HSD2 的 IC50 值 > 30 μM（人 11β-HSD2 负责针对人 11β-HSD1 的逆反应）。JTT-654 通过抑制脂肪组织和肝脏 11β-HSD1 改善胰岛素抵抗和非肥胖 2 型糖尿病。

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JTT-654 Chemical Structure

JTT-654 Chemical Structure

CAS No. : 916828-66-5

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JTT-654 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]
体外研究
(In Vitro)

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.

JTT-654 相关抗体:
体内研究
(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: 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.
分子量

530.58

Formula

C28H33F3N4O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

JTT-654 相关分类

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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.

Keywords:

JTT-654916828-66-5JTT654JTT 65411β-HSD11beta-HSD11β-hydroxysteroid dehydrogenases11 beta-hydroxysteroid dehydrogenasenon-obese type 2 diabetesorally active3T3-L1adipocytesInhibitorinhibitorinhibit

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