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Art. -Nr.: HY-182769

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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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CAS. Nr.: 3066979-01-6
Formel: C₂₃H₁₉F₃N₆O₂
Molecular Weight:468.43

Speicherung:

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

TRβ agonist-4 Chemical Structure

CAS. Nr.: 3066979-01-6

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Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	MRT_0-inf	CL/F	V_z/F	AUC_0-t	AUC_0-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 %

In Vivo

The racemate of TR-β agonist-4 (Compound 1) (5 mg/kg) dose-dependently reduces serum total cholesterol and low-density lipoprotein cholesterol levels in hyperlipidemic mice induced by a high-fat diet^[1].
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

CAS. Nr. 3066979-01-6
Molecular Weight 468.43
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wang Zhenyu, et al. CRYSTAL FORM OF TR-β SELECTIVE AGONIST, PREPARATION METHOD, AND USE. WO2026050911A1. 2024-09-04.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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