S84389 |
Sobetirome |
源葉(MedMol) | 98% |
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- 產(chǎn)品描述: Sobetirome is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM).
- 靶點(diǎn): Thyroid hormone receptor(THR);Thyroidhormonereceptor(THR)
- 體內(nèi)研究:
Four weeks following injection, mice were fed 5 mg/kg GC-1 or basal diet for 10 or 21 days. Treatment with GC-1 for 10 or 21 days led to a significant reduction in tumor burden. GC-1 treatment reduced serum cholesterol levels by 25% and serum triglycerides by 75% in chow-fed mice and also attenuated diet-induced hypercholesterolemia. GC-1 (50 or 100 mug/100 g body weight) strongly stimulates rat hepatocyte proliferation in the absence of tissue injury. GC-1 also induced massive pancreatic cell proliferation
- 動(dòng)物實(shí)驗(yàn): Briefly, 20 μg of a pT3-EF5α-hMet-V5 and pT3-EF5α-S45Y-β-catenin-Myc combination along with the transposase in a ratio of 25:1 were diluted in 2 mL of normal saline (0.9% NaCl), filtered through a 0.22-μm filter, and injected into the lateral tail vein of 23 FVB mice that were around 6 weeks old, in 5 to 7 seconds. These mice are referred henceforth as hMet-mutant-β-catenin mice. Four weeks after injection, hMet-mutant-β-catenin mice were randomized into two groups. One group was kept on a basal diet (n = 12), and another group was switched to a GC-1–supplemented diet (5 mg/kg of diet) (n = 11). Animals on control diet were sacrificed at either 21 days (n = 8) or 10 days (n = 4) after initiation of the diet. Similarly, animals on the GC-1 diet were sacrificed at either 21 days (n = 7) or 10 days (n = 4) after initiation of the diet. The animals were given access to food and water ad libitum with a 12-hour light/dark daily cycle. One intraperitoneal injection of bromodeoxyuridine (BrdU) was performed on day 9
- 參考文獻(xiàn):
1. Gierach I, et al. Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors α-1 and β-1. FEBS Open Bio. 2012 Aug 15;2:247-53. 2. Johansson L, et al. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice. Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10297-302. 3. Columbano A, et al. The thyroid hormone receptor-beta agonist GC-1 induces cell proliferation in rat liver and pancreas. Endocrinology. 2006 Jul;147(7):3211-8. 4.Puliga E, et al. Thyroid Hormone Receptor-β Agonist GC-1 Inhibits Met-β-Catenin-Driven Hepatocellular Cancer. Am J Pathol. 2017 Nov;187(11):2473-2485.
- 溶解性: Soluble in DMSO、Ethanol
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.045 ml 15.225 ml 30.451 ml 5 mM 0.609 ml 3.045 ml 6.09 ml 10 mM 0.305 ml 1.523 ml 3.045 ml 50 mM 0.061 ml 0.305 ml 0.609 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)