CHIR99021高效抑制剂

CHIR99021
252917-06-9

￥450 2mg 起订

江苏更新日期：2024-04-23

南京百鑫德诺生物科技有限公司

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产品详情:

中文名称：: CHIR99021

英文名称：: CHIR99021

CAS号：: 252917-06-9

品牌：: Adooq

保存条件：: -80°C, 6 months; -20°C, 1 month;

纯度规格：: 99%

产品类别：: 生物试剂

货号：: A10199

用途范围：: 科研实验

CHIR99021是一种GSK-3α和GSK-3β抑制剂，IC50值分别为10和6.7 nM。

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.
实验	N/A
特征	N/A

相关实验数据(此数据来自于公开文献,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

3-Pyridinecarbonitri;CAS号252917-06-9 ;CHIR99021;

Adooq( http://www.adooq.cn, 南京百鑫德诺生物科技有限公司) 是Adooq Bioscience 在中国设立的全资子公司，全面负责其在中国地区的业务运营，包括产品销售，售后服务及技术支持. Adooq目前提供超过2000种包括GPCR配体、神经递质、离子通路和信号抑制物等在内的化学小分子和多肽等生命科学研究试剂。 Adooq拥有全球领先的小分子抑制剂和有机天然活性产物的生产工艺技术平台。每年新增小分子化合物300-500种，新增天然活性产物500余种，已成为多个跨国制药企业，生物科技公司，医院及各大临床诊断实验室在小分子抑制剂研究领域的全球首选供应商。

成立日期	(11年)
注册资本	100万元整
员工人数	10-50人
年营业额	￥ 100万以内
经营模式	试剂
主营行业	化学试剂,生物活性小分子