2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. 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).

For research use only. We do not sell to patients.

TRβ agonist-4

TRβ agonist-4 Chemical Structure

CAS No. : 3066979-01-6

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TRβ agonist-4 Related Antibodies

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Description

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)[1].

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.

TRβ agonist-4 Related Antibodies
Parmacokinetics
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 %
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.
Molecular Weight

468.43

Formula

C23H19F3N6O2
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TRβ agonist-4 Related Classifications

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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:

TRβ agonist-43066979-01-6TRβ agonist4TRβ agonist 4Thyroid Hormone ReceptorTHRnon-alcoholic steatohepatitisSLCO1B1TRαHEK293T cellsTHR-αhigh-fat diet induced hyperlipidemia miceHFD+CCl 4 induced non-alcoholic steatohepatitis miceTHR-βTRβInhibitorinhibitorinhibit

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