| Bioactivity | TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of 21 nM. TRβ agonist 1 can be used for researching dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH)[1]. |
| Target | EC50: 21.0 nM , 1344.0 nM |
| Invitro | TRβ agonist 1 (compound 16g) (1, 3, 10 μM; 24 hours) reduces lipid accumulation and cholesterol levels by triglyceride (TG) and total cholesterol (TC) analyses in HepG2 cells and primary mouse hepatocytes; also reduces the total lipid accumulation at 10 μM[1].TRβ agonist 1 (10 μM; 24 hours) induces a significant enhancement of the p-AMPK/AMPK ratio, the p-ACC/ACC ratio, and CPT1 levels[1].TRβ agonist 1 (0.01, 0.1, 1 and 10 μM; 24 hours) does not display significant cellular toxicity on multiple cell lines (HepG2, 22Rv1, A549, MCF7, MDA-MB-231, HFL-1, and BxPC-3) at concentrations up to 10 μM[1]. |
| Name | TRβ agonist 1 |
| CAS | 2770681-85-9 |
| Formula | C29H25FN2O8 |
| Molar Mass | 548.52 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Li Q, et al. Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist. J Med Chem. 2022;65(10):7193-7211. |
TRβ agonist 1
CAS: 2770681-85-9 F: C29H25FN2O8 W: 548.52
TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of
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