CHIR 99021 trihydrochloride

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
100mg	询价

化学性质

Physical Appearance	Off White solid
Storage	Store at -20°C
M.Wt	574.72
Formula	C₂₂H₁₈Cl₂N₈·3HCl
Solubility	insoluble in EtOH; ≥21.87 mg/mL in DMSO; ≥32.45 mg/mL in H2O
Chemical Name	(Z)-6-((2-((E)-(4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2(1H)-ylidene)amino)ethyl)imino)-1,6-dihydropyridine-3-carbonitrile trihydrochloride
Canonical SMILES	CC(N1)=CN=C1C(C(C2=C(Cl)C=C(Cl)C=C2)=N/3)=CNC3=N/CC/N=C4C=CC(C#N)=CN/4.Cl.Cl.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

CHIR 99021 trihydrochloride is hydrochloride of CHIR 99021, which inhibits GSK-3α and GSK-3β with IC50 values of 10 nM and 6.7 nM. GSK-3 is a serine/threonine kinase, responsible for phosphorylating either the serine or threonine residues of its substrates. This phosphorylation process is involved in various key biological processes, including gene transcription, protein synthesis, cell signaling, cellular transport, proliferation, apoptosis, intracellular communication and glucose regulation.

References:

1. Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52(3): 588-595.

2. Pandey MK, DeGrado TR. Glycogen synthase kinase-3 (GSK-3)-targeted therapy and imaging. Theranostics, 2016, 6(4): 571-593.

3. Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.

试验操作

Cell experiment:[3]
Cell lines	INS-1E cells
Reaction Conditions	0 ~ 20 μM CHIR 99021 for 24 h incubation
Applications	CHIR 99021 increased the rate of proliferation of INS-1E cells in a dose-dependent manner, with the rate of proliferation reaching a maximum in the presence of 2.5 ~ 10 μM CHIR 99021. Moreover, CHIR 99021 also dose-dependently counteracted INS-1E cell death induced by high glucose and high palmitate.
Animal experiment:[2]
Animal models	Male ZDF rats with type 2 diabetes
Dosage form	16, 30 or 48 mg/kg Orally
Applications	In ZDF rats with type 2 diabetes, a single oral dose of CHIR 99021 at 30 mg/kg rapidly lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3 ~ 4 hours after administration, while plasma insulin remained at or below control levels. Moreover, oral administration of CHIR 99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats substantially improved glucose tolerance, with 14% and 33% reduction in plasma glucose.
Note	The technical data provided above is for reference only.
	References: 1. Ring DB, Johnson KW, Henriksen EJ, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003, 52(3): 588-595. 2. Pandey MK, DeGrado TR. Glycogen synthase kinase-3 (GSK-3)-targeted therapy and imaging. Theranostics, 2016, 6(4): 571-593. 3. Mussmann R, Geese M, Harder F, et al. Inhibition of GSK3 promotes replication and survival of pancreatic beta cells. Journal of Biological Chemistry, 2007, 282(16): 12030-12037.