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Product Name:THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 CAS:251310-57-3 Purity:95+% Package:1g;5g
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| THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 Basic information |
Product Name: | THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 | Synonyms: | THYROID HORMONE RECEPTOR ANTAGONIST, 1-850;TR ANTAGONIST 1-850;2-(2-(-(4-NITROPHENYL)-4-PIPERIDINYLIDENE)ACETYL)-N-(3-(TRIFLUOROMETHYL) PHENYL)-1-HYDRAZINE CARBOXAMIDE;1-[[2-[1-(4-nitrophenyl)piperidin-4-ylidene]acetyl]amino]-3-[3-(trifluoromethyl)phenyl]urea;Acetic acid, 2-[1-(4-nitrophenyl)-4-piperidinylidene]-, 2-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]hydrazide | CAS: | 251310-57-3 | MF: | C21H20F3N5O4 | MW: | 463.41 | EINECS: | | Product Categories: | | Mol File: | Mol File | ![THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 Structure](StructureFile/ChemBookStructure8/GIF/CB8468369.gif) |
| THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 Chemical Properties |
density | 1.464±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | ≤0.5mg/ml in ethanol;50mg/ml in DMSO;50mg/ml in dimethyl formamide | form | crystalline solid | pka | 9.75±0.43(Predicted) |
| THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 Usage And Synthesis |
Description | The activity of the thyroid hormones, L-thyroxine (T4; ) and 3,3'',5-triiodo-L-thyronine (T3; ), is mediated by thyroid hormone nuclear receptors TRα and TRβ. Gene knockout studies in mice indicate that TRα modulates the effect of thyroid hormone on calorigenesis and on the cardiovascular system, while TRβ plays a role in the development of the auditory system and in the negative feedback of thyroid stimulating hormone by T3 in the pituitary. Thyroid hormone receptor antagonist (1-850) competitively blocks T3 binding to both TRα and TRβ (IC50s = 1.5 μM), demonstrating ~1,000-fold lower affinity for TRα in intact cells compared with T3. This compound is specific, showing no effect on the activity of the related retinoic acid receptor α. | target | thyroid hormone receptor | IC 50 | 1.5 μm | references | [1] schapira m, raaka b m, das s, et al. discovery of diverse thyroid hormone receptor antagonists by high-throughput docking[j]. proceedings of the national academy of sciences of the united states of america, 2003, 100(12): 7354-7359. |
| THYROID HORMONE RECEPTOR ANTAGONIST, 1-850 Preparation Products And Raw materials |
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