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- 文献和实验
- 技术资料
- CAS号:
211110-63-3
- 规格:
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥756.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥334.0 |
| 规格: | 5mg | 产品价格: | ¥713.0 |
| 规格: | 10mg | 产品价格: | ¥1088.0 |
| 规格: | 25mg | 产品价格: | ¥2144.0 |
| 规格: | 50mg | 产品价格: | ¥3336.0 |
| 规格: | 100mg | 产品价格: | ¥4744.0 |
| 规格: | 200mg | 产品价格: | ¥6584.0 |
Product Introduction
Bioactivity
| 名称 | Sobetirome |
| 描述 | Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM). |
| 动物实验 | 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 during 10 days of GC-1 or basal diet treatment, and livers were harvested 24 hours later [2]. |
| 体外活性 | GC-1特意设计用于选择性地结合于TRβ(EC50:TRα-1为0.58 μM,TRβ-1为0.16 μM)[1]。作为甲状腺激动剂,GC-1通过Wnt/β-catenin信号通路诱导肝细胞增殖,可能在急性及慢性肝功能不全中促进再生[2]。 |
| 体内活性 | 注射四周后,小鼠被喂养含5 mg/kgSobetirome或基础饮食,持续10天或21天。Sobetirome的治疗在10天或21天内显著降低了肿瘤负担[2]。Sobetirome治疗使得标准饮食下的小鼠血清胆固醇水平降低了25%,血清甘油三酯降低了75%,同时减轻了饮食引起的高胆固醇血症[3]。Sobetirome(50或100 mug/100 g体重)显著促进了大鼠肝细胞在无组织损伤的情况下的增殖,并导致了大量的胰腺细胞增殖[4]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+90% Saline : < 10 mg/mL (30.45 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. DMSO : 145 mg/mL (441.53 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (30.45 mM), Solution. Ethanol : 30 mg/mL (91.35 mM), Sonication is recommended. |
| 关键字 | TRβ | Thyroidhormonereceptor(THR) | Thyroidhormonereceptor | Thyroid hormone receptor(THR) | Thyroid Hormone Receptor | THR | Sobetirome | QRX431 | QRX 431 | Inhibitor | inhibit | IACS010759 | IACS 010759 |
| 相关产品 | L-Thyroxine sodium | Iopanoic acid | Azetirelin | Carbimazole | Methimazole | Resmetirom | PCO371 | 2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE | DS08210767 | Eneboparatide | Octinoxate | Tiratricol |
| 相关库 | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Failed Clinical Trials Compound Library | Endocrinology-Hormone Compound Library | NO PAINS Compound Library | Nuclear Receptor Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Pediatric Drug Library | Target-Focused Phenotypic Screening Library | Human Metabolite Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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