产品名称

英文名称：AZD1080

同义词

AZD1080、612487-72-6、AZD-1080、2-hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile、AZ-11548415、0TII45R8IJ、AZD 1080、UNII-0TII45R8IJ、2-Hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1H-indole-5-carbonitrile、2-Hydroxy-3-[5-(4-morpholiny、2-羟基-3-[5-[(吗啉-4-基)甲基]吡啶-2-基]-1H-吲哚-5-甲腈

产品性质

CAS编号：612487-72-6

分子式：C19H18N4O2

分子量：334.37

PubChem编号：135564570

别名：2-羟基-3-[5-[(吗啉-4-基)甲基]吡啶-2-基]-1H-吲哚-5-甲腈

英文别名：AZD1080|612487-72-6|AZD-1080|2-hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile|AZ-11548415|0TII45R8IJ|AZD 1080|UNII-0TII45R8IJ|2-Hydroxy-3-(5-((morpholin-4-yl)methyl)pyridin-2-yl)-1H-indole-5-carbonitrile|2-Hydroxy-3-[5-(4-morpholiny

规格或纯度：≥98%

英文名称：AZD1080

生化机理：DescriptionIC50 Value 31 nM [1]AZD1080 is a potent and selective GSK3 inhibitor that demonstrates peripheral target engagement in Phase 1 clinical studies.in vitro AZD1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. Interestingly, subchronic but not acute administration with AZD1080 reverses MK-801-induced deficits, measured by long-term potentiation in hippocampal slices and in a cognitive test in mice, sμggesting that reversal of synaptic plasticity deficits in dysfunctional systems requires longer term modifications of proteins downstream of GSK3β signaling [1].in vivo AZD1080 reverses MK-801-induced impairments in mouse model of cognition. AZD1080 treatment significantly prevents MK-801-induced deficits at both time-points (*p < 0.05; **p < 0.01).Data are presented as mean _ SEM (n = 9-12 subjects/group). [1]Clinical trial Phase 1

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：卖完停产，不再备货

产品介绍：AZD1080是口服活性的可通透脑屏障的GSK3α和GSK3β抑制剂，Ki分别为6.9 nM和31 nM。AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor of GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2.

IUPAC Name：2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indole-5-carbonitrile

INCHI：InChI=1S/C19H18N4O2/c20-10-13-1-3-16-15(9-13)18(19(24)22-16)17-4-2-14(11-21-17)12-23-5-7-25-8-6-23/h1-4,9,11,22,24H,5-8,12H2

InChi Key：BLTVBQXJFVRPFK-UHFFFAOYSA-N

Canonical SMILES：C1COCCN1CC2=CN=C(C=C2)C3=C(NC4=C3C=C(C=C4)C#N)O

Isomeric SMILES：C1COCCN1CC2=CN=C(C=C2)C3=C(NC4=C3C=C(C=C4)C#N)O

PubChem CID：135564570

CAS Registry No.：612487-72-6

Reactome Reaction：R-HSA-9687724

Reactome Drug：R-ALL-9687660

溶解性：DMSO 52 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

产品包装