购物车
- 全部删除
- 您的购物车当前为空
Sobetirome (IACS-010759) 是一种甲状腺激素受体 β (TRβ) 激动剂,能够选择性的结合到TRβ-1(EC50:0.16 μM)。
Sobetirome (IACS-010759) 是一种甲状腺激素受体 β (TRβ) 激动剂,能够选择性的结合到TRβ-1(EC50:0.16 μM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 398 | 现货 | |
5 mg | ¥ 892 | 现货 | |
10 mg | ¥ 1,360 | 现货 | |
25 mg | ¥ 2,680 | 现货 | |
50 mg | ¥ 4,170 | 现货 | |
100 mg | ¥ 5,930 | 现货 | |
200 mg | ¥ 8,230 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 945 | 现货 |
产品描述 | Sobetirome (IACS-010759) is a selective agonist of thyroid hormone receptor β (TRβ) and binds selectively to TRβ-1 (EC50: 0.16 μM). |
靶点活性 | TRα 1:0.58 μM (EC50), TRβ 1:0.16 μM (EC50) |
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]。 |
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]. |
别名 | IACS-010759, GC1, QRX-431, GC-1, GC 1 |
分子量 | 328.4 |
分子式 | C20H24O4 |
CAS No. | 211110-63-3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 30 mg/mL (91.4 mM) Ethanol: 30 mg/mL | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.