| Bioactivity | TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ, respectively. |
| Target | IC50: 36 nM (Thyroid hormone α), 22 nM (Thyroid hormone α) |
| Invitro | TR antagonist 1 displays high affinity for both thyroid hormone TRα and TRβ (IC50=36 and 22 nM, respectively). TR antagonist 1 acts as a full antagonist in the TRAFR cell assay and the IC50 32 nM for both TRAFα1 and TRAFβ1[1]. |
| In Vivo | TR antagonist 1 treatment lowers heart rate and shows a possible trend toward an increase of low-density lipoprotein cholesterol (LDL-C) in the cholesterol fed rat model[1]. |
| Name | TR antagonist 1 |
| CAS | 500794-88-7 |
| Formula | C25H23Br2NO4 |
| Molar Mass | 561.26 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Koehler K, et al. Thyroid receptor ligands. 6. A high affinity "direct antagonist" selective for the thyroid hormone receptor. J Med Chem. 2006 Nov 16;49(23):6635-7. |
TR antagonist 1
CAS: 500794-88-7 F: C25H23Br2NO4 W: 561.26
TR antagonist 1 is a high-affinity thyroid hormone receptor (TR) antagonist with IC50s of 36 and 22 nM for TRα and TRβ
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