型号:
产品价格:电议      采购度:1605      原产地:美洲
发布时间:2021/7/24 5:12:52 所属地区:上海 上海市
简要描述:
AZD1080 是一种有效的选择性 GSK3 抑制剂。AZD1080 抑制重组人 GSK3α 和 GSK3β,pKi (IC50) 分别为 ( nM) 和 (31 nM)。
标签:azd1080
产品详情
MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 612487-72-6
MCE 站:AZD1080
产品活性:AZD1080 是一种有效的选择性 GSK3 抑制剂。AZD1080 抑制重组人 GSK3α 和 GSK3β,pKi (IC50) 分别为 8.2 (6.9 nM) 和 7.5 (31 nM)。
研究领域:PI3K/Akt/mTOR | Stem Cell/Wnt
作用靶点:GSK-3
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 LiCl.
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 p<0.01 at 15 μmol/kg) in mice, raising the hypothesis that longer treatment may be required to prime the synapses to function effectively.
相关产品:Bioactive Compound Library Plus | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Anti-Pancreatic Cancer Compound Library | CHIR-99021 | SB 216763 | AR-A014418 | TDZD-8 | Kenpaullone | GSK 3 Inhibitor IX | Cromolyn sodium | R547 | SB 415286 | IM-12 | Indirubin-3'-monoxime | 1-Azakenpaullone | AZD2858 | BIO-acetoxime | CP21R7 | Bikinin | GNF4877 | GSK-3β inhibitor 1 | hSMG-1 inhibitor 11j | TCS 21311 | BIP-135 | 5-Iodo-indirubin-3'-monoxime | Alsterpaullone | GSK-3 inhibitor 1 | GSK-3β inhibitor 2 | Manzamine A hydrochloride | 2B-(SP)
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。
更新时间:2024/1/2 10:14:41
留言咨询
温馨提示
1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。
相关新闻
相关产品