Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Laduviglusib trihydrochloride (CT99021 trihydrochloride) 是一种选择性糖原合成酶激酶 3 (GSK-3) 抑制剂,对 GSK-3α 和 GSK-3β 的 IC50 分别为 10 nM 和 6.7 nM。 Laduviglusib trihydrochloride 抑制人 GSK-3β,Ki 为 9.8 nM。 Laduviglusib trihydrochloride 是 Wnt/β-catenin 信号通路的激活剂。 Laduviglusib trihydrochloride 诱导自噬。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 372 | 现货 | ||
2 mg | ¥ 538 | 现货 | ||
5 mg | ¥ 781 | 现货 | ||
10 mg | ¥ 1,280 | 现货 | ||
25 mg | ¥ 2,390 | 现货 | ||
50 mg | ¥ 3,690 | 现货 | ||
100 mg | ¥ 5,320 | 现货 | ||
500 mg | ¥ 10,800 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 937 | 现货 |
产品描述 | Laduviglusib trihydrochloride (CT99021 trihydrochloride) is a selective glycogen synthase kinase 3 (GSK-3) inhibitor with IC50s of 10 nM and 6.7 nM for GSK-3α and GSK-3β. Laduviglusib trihydrochloride inhibits human GSK-3β with a Ki of 9.8 nM. Laduviglusib trihydrochloride is an activator of Wnt/β-catenin signaling. Laduviglusib trihydrochloride induces autophagy. |
靶点活性 | GSK-3α:10 nM, GSK-3β:6.7 nM, CDC2:8800 nM |
体外活性 | Laduviglusib trihydrochloride(10 μM) lowers the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% with an IC50 of 4.9 μM[2]. Laduviglusib trihydrochloride shows >500-fold selectivity over ERK2, CDC2, and other protein kinases. Laduviglusib trihydrochloride specifically inhibits GSK3β and GSK3α with IC50s of 5nM and 10nM in vitro kinase assays[4]. |
体内活性 | Oral administration of Laduviglusib trihydrochloride(16 mg/kg and 48 mg/kg) rapidly reduces plasma glucose with a maximal reduction of nearly 150 mg/dl in ZDF rats[1]. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride (2 mg/kg) improves survival after 14.5 Gy abdominal irradiation. Laduviglusib trihydrochloride inhibits crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride blocks apoptosis, increases Lgr5+ cell survival and prevents the reduction of Olfm4, Lgr5 and CD44[5]. |
别名 | CT99021 trihydrochloride, CHIR 99021 trihydrochloride, CHIR 99021 trihydrochloride (252917-06-9 free base) |
分子量 | 574.72 |
分子式 | C22H21Cl5N8 |
CAS No. | 1782235-14-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 17.1 mg/mL (29.8 mM), Sonication and heating are recommended.
DMSO: 28.8 mg/mL (50.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 1.74 mL | 8.6999 mL | 17.3998 mL | 43.4994 mL |
5 mM | 0.348 mL | 1.74 mL | 3.48 mL | 8.6999 mL | |
10 mM | 0.174 mL | 0.87 mL | 1.74 mL | 4.3499 mL | |
20 mM | 0.087 mL | 0.435 mL | 0.87 mL | 2.175 mL | |
DMSO | 50 mM | 0.0348 mL | 0.174 mL | 0.348 mL | 0.87 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Laduviglusib trihydrochloride 1782235-14-6 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells GSK-3 Wnt/beta-catenin 252917-06-9 free base CHIR 99021 Trihydrochloride CT99021 trihydrochloride Laduviglusib CHIR99021 Trihydrochloride CT99021 Trihydrochloride CT-99021 Trihydrochloride CT 99021 Trihydrochloride CT99021 CHIR 99021 CHIR 99021 trihydrochloride CHIR 99021 trihydrochloride (252917-06-9 free base) 252917-06-9 CHIR99021 CHIR-99021 CHIR-99021 Trihydrochloride CT-99021 Laduviglusib Trihydrochloride CT 99021 Inhibitor inhibitor inhibit