CHIR-99021 (GSK-3抑制剂)
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产品编号 SF2708-10mM
数量
¥ 257.00
产品包装:
10mM×0.2ml 5mg 25mg
产品简介
使用说明
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化学信息:

化学名 6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile
简称 CHIR-99021
别名 Chir 99021, Chir-99021, Chir99021, CT 99021, CT-99021, CT99021
中文名 N/A
化学式 C22H18Cl2N8
分子量 465.34
CAS号 252917-06-9
纯度 98%
溶剂/溶解度 Water<1mg/ml; DMSO78mg/ml; Ethanol<1mg/ml
溶液配制 5mg加入1.07ml DMSO,或者每4.65mg加入1ml DMSO,配制成10mM溶液。SF2708-10mM用DMSO配制。

生物信息:

产品描述 CHIR-99021 (CT99021)是一种GSK-3α和GSK-3β抑制剂,IC50分别为10nM和6.7nM。
信号通路 PI3K/Akt/mTOR; Stem Cells & Wnt
靶点 GSK-3β GSK-3α
IC50 6.7nM 10nM
体外研究 CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763μM.
体内研究 Oral administration of CHIR-99021 at 30mg/kg enhances glucose metabolism in a rodent model of type 2 diabetes, with a maximal plasma glucose reduction of nearly 150mg/dl 3-4 hours after administration, while plasma insulin remains at or below control levels. Oral administration of CHIR-99021 at 16 or 48mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16mg/kg and 48mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge.
临床实验 N/A
特征 N/A

相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):

酶活性检测实验
方法 N/A
细胞实验
细胞系 Insulin receptor-expressing CHO-IR cells; Primary rat hepatocytes
浓度 0.01-10μM
处理时间 30 min
方法 CHO-IR cells expressing human insulin receptor are grown to 80% confluence in Hamm's F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1×106 cells/well in 2ml of medium without fetal bovine serum. After 24h, medium is replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37℃. Cells are lysed and centrifuged 15 min at 4℃/14000g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5mMol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.
动物实验
动物模型 Female db/db mice; Male ZDF rats
配制 HCl salts formulated
剂量 8-48mg/kg
给药方式 oral administration
参考文献:
1. Ring DB, et al. Diabetes. 2003, 52(3), 588-595.
包装清单:
产品编号 产品名称 包装
SF2708-10mM CHIR-99021 (GSK-3抑制剂) 10mM×0.2ml
SF2708-5mg CHIR-99021 (GSK-3抑制剂) 5mg
SF2708-25mg CHIR-99021 (GSK-3抑制剂) 25mg
说明书 1份

保存条件:
        -20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。

注意事项:
本产品对人体有毒,操作时请特别小心,并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用,不得用于临床诊断或治疗,不得用于食品或药品,不得存放于普通住宅内。
为了您的安全和健康,请穿实验服并戴一次性手套操作。
使用说明:
1.收到产品后请立即按照说明书推荐的条件保存。使用前可以在2,000-10,000g离心数秒,以使液体或粉末充分沉降至管底后再开盖使用。
2.对于10mM溶液,可直接稀释使用。对于固体,请根据本产品的溶解性及实验目的选择相应溶剂配制成高浓度的储备液(母液)后使用。
3.具体的最佳工作浓度请参考本说明书中的体外、体内研究结果或其它相关文献,或者根据实验目的,以及所培养的特定细胞和组织,通过实验进行摸索和优化。
4.不同实验动物依据体表面积的等效剂量转换表请参考如下网页:http://www.beyotime.com/support/animal-dose.htm
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