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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 916828-66-5
- 分子式: C28H33F3N4O3
- 分子量:530.58
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
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]
体外実験
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. Further protocols information, click here.
体内実験
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.
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Animal Model:SD rats (8 weeks old)[1]
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Dosage:1, 3, or 10 mg/kg
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Administration:Orally, single administration
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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.
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Animal Model:Male Wistar rats (7-week-old)[1]
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Dosage:1, 3, 10 mg/kg
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Administration:Orally, once daily for 4 d, Cortisone was administered 1 h after JTT-654 administration on each day of dosing.
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Result:Significantly attenuated the increase in fasted plasma glucose and insulin levels in a dose-dependent manner.
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Animal Model:Non-obese type 2 diabetic Goto-Kakizaki (GK) Rats (8-week-old, male)[1]
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Dosage:1.5, 5, 15 mg/kg
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Administration:Orally, twice daily, for 19 d
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Result:Significantly reduced fasting plasma glucose and insulin levels, enhanced insulin-stimulated glucose oxidation in adipose tissue, and suppressed hepatic gluconeogenesis.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 916828-66-5
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分子量 530.58
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分子式 C28H33F3N4O3
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Large-size fat particle sorting
Large-size fat particle sorting is widely used to isolate cells up to 200 μm in diameter. Single-cell flow sorting will allow greater insight into adipocyte heterogeneity by identifying gene expression, protein composition, and metabolic signatures at the single-cell level.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
純度とドキュメンテーション
参考文献
[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. [Content Brief]
[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. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)