TRβ agonist-4
TRβ agonist-4 is an orally bioavailable, liver-targeted selective agonist of hTHR-β (EC50=6.0 nM), with a 105.3-fold selectivity over THR-α. TRβ agonist-4 exists in multiple crystal forms, including Form A, Form B, Form C, Form D, Form E, as well as an amorphous form. TRβ agonist-4 can be used for research related to non-alcoholic steatohepatitis (NASH).
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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: 3066979-01-6
- 分子式: C23H19F3N6O2
- 分子量:468.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
The racemate of TR-β agonist-4 (Compound 1) shows significantly enhanced THR-β activation activity in HEK293T cells overexpressing the liver-specific transporter SLCO1B1, with an EC50 as low as 13.4 nM at 24 h and a liver-targeting fold of 24.9 (superior to MGL-3196 (HY-12216))[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | MRT0-inf | CL/F | Vz/F | AUC0-t | AUC0-inf | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey[1] | 5 mg/kg | p.o. | 2.20 h | 4 h | 68.4 ng/mL | 5.16 h | 237 mL/min/kg | 45.9 L/kg | 386 ng·h/mL | 402 ng·h/mL | 4.03 % |
The racemate of TR-β agonist-4 (Compound 1) at a dose of 0.5 mg/kg significantly reduces hepatic TG and TC levels as well as NASH scores in mice with nonalcoholic steatohepatitis induced by HFD+CCl4, and its efficacy is comparable to that of 10 mg/kg MGL-3196 (HY-12216)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3066979-01-6
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分子量 468.43
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分子式 C23H19F3N6O2
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SMILES
FC(F)(F)[C@H](C(C1=N2)=CNC1=CC=C2CC3=C(C=C(N4N=C(C(NC4=O)=O)C#N)C=C3C)C)C
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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.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TRβ agonist-4 関連分類
HY-182769 関連分類
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