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).
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3066979-01-6
- Fòrmula: C23H19F3N6O2
- Peso molecular:468.43
-
Almacenamiento:
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]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
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.
Chemical Information
-
No. CAS 3066979-01-6
-
Peso molecular 468.43
-
Fòrmula C23H19F3N6O2
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRβ agonist-4 Related Classifications
HY-182769 Related Classifications
Powered by Bioz