Immunoway/AZD1080/10mg 50mg 100mg/MC0211
市场价：
¥14000.00
美元价：
7000.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
AZD1080
- Catalog No.：MC0211
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 612487-72-6
- MolecularFormula：
- C19H18N4O2
- Purity：
- >98%
- Target：
- GSK-3
- IC50：
- IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
- In Vitro：
- AZD1080 shows selectivity against cdk2 (pKi=5.9; 1150 nM; 37-fold), cdk5 (pKi=6.4; 429 nM; 14-fold), cdk1 (pKi=5.7; 1980 nM; 64-fold) and Erk2 (pKi< 5;="">10 μM; >323-fold). AZD1080 (at 10 μM) is also evaluated for pan-kinase selectivity and showed good overall selectivity versus 23 kinases, as well as against 65 different receptors, enzymes and ion channels in MDS Pharma screen (< 50%="" effect="" at="" 10="" μm="" azd1080).="" concentration-dependent="" inhibition="" of="" tau="" phosphorylation="" is="" observed="" for="" azd1080="" (ic50="324" nm)="" and="" the="" non-selective="" reference="" gsk3="" inhibitor="" licl="" (ic50="1.5" mm)="" indicating="" that="" azd1080="" is="" several="" orders="" of="" magnitude="" more="" potent="" than="">
- In Vivo：
- The pharmacokinetic analysis in blood after oral administration revealed that AZD1080 has a good oral bioavailability in rats (15-24%) with a half-life of 7.1 h, making AZD1080 attractive for further in vivo testing. The subchronic (3 days) oral treatment with AZD1080 at 4 or 15 μmol/kg significantly blocked the MK-801-induced memory deficit (AZD1080 vs. MK-801, p<0.05 at="" 4="" μmol/kg="" and=""><0.01 at="" 15="" μmol/kg)="" in="" mice,="" raising="" the="" hypothesis="" that="" longer="" treatment="" may="" be="" required="" to="" prime="" the="" synapses="" to="" function="">
- Fields：
- AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against CDK2, CDK5, CDK1 and Erk2. IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
- Specificity：
- Target:GSK-3. Fields: AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity agai
- Source：
- Rabbit
- Dilution：
- IC50: 6.9 nM (GSK3α), 31 nM (GSK3β)[1]pKi: 8.2 (GSK3α), 7.5 (GSK3β)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- AZD 1080,AZD-1080
- MolecularWeight(Da)：
- 334.37
- References：
- [1]. Georgievska B, et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013 May;125(3):446-5
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