型号:
产品价格:电议      采购度:1310      原产地:美洲
发布时间:2022/1/21 16:23:23 所属地区:国外 国外
简要描述:
AMG-221 是 11β-羟基类固醇脱氢酶 1 (11β-HSD1) 抑制剂, Ki 为 nM,IC50 为 nM。AMG-221 可用于 2 型糖尿病的研究。
标签:amg-221
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. : 1095565-81-3
MCE 站:AMG-221
产品活性:AMG-221 是 11β-羟基类固醇脱氢酶 1 (11β-HSD1) 抑制剂, Ki 为 12.8 nM,IC50 为 10.1 nM。AMG-221 可用于 2 型糖尿病的研究。
研究领域:Others
作用靶点:Others
In Vitro: AMG-221 shows selectivity over 11β-HSD2, 17β-HSD1, and glucocorticoid receptor (GR) (IC50?values for all assays are >10 μM).
In Vivo: AMG-221 (25 or 50 mg/kg;?b.i.d.; orally gavaged) inhibits 11β-HSD1 activity in DIO mice. At the end of the study, fed blood glucose shows statistically significant reduction in comparison to the vehicle group. On day 14 and after a 12 h fast, glucose tolerance is slightly improved in the AMG-221?treatment groups compared with the vehicle group.
11β-HSD1 activity is inhibited by 33%, 55%, and 47% in the inguinal fat at 4 h after?AMG-221?is orally gavaged at 5, 15, and 50 mg/kg, respectively. At 8 h, the 11β-HSD1 activity in the inguinal fat of the 5 mg/kg group has returned to a level (?10% inhibition) close to that in the control animals treated with vehicle, but there is still significant inhibition in the 15 and 50 mg/kg groups (36% and 39% inhibition, respectively).
AMG-221?has a good bioavailability in mouse, rat, and dog. However, the bioavailability in monkey is low.
AMG-221 exhibits moderate oral bioavailability (male CD1 mouse 31%) following oral administration (10 mg/kg).
AMG-221 exhibits terminal elimination half-life (male CD1 mouse 3.32 h) due to high plasma clearance (3.31 L/h/kg) combined with large volumes of distribution (0.9 L/kg) following intravenous administration (2 mg/kg).
相关产品:PEG300 | SBE-β-CD | Corn oil | Tween 80 | D-Lin-MC3-DMA | Polyethylene glycol 12-hydroxystearate | Lipopolysaccharides | JC-1 | (2-Hydroxypropyl)-β-cyclodextrin | Digitonin | Methyl-β-cyclodextrin | 5-Ph-IAA | CFSE | Tocofersolan | Biotin | O-Propargyl-Puromycin | Yoda 1 | 3X FLAG peptide TFA | DTT | GsMTx4 TFA | Monocrotaline | Cremophor EL | Thiazolyl Blue | FLAG peptide | IPTG | Nile Red | Sodium carboxymethyl cellulose (Viscosity:800-1200 mPa.s) | D-Luciferin potassium | Phosal 50 PG
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 染料试剂 | PROTAC | 同位素标记物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
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 10:19:40
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