产品描述
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. : 306288-04-0
MCE 国际站：AVE 0991 sodium salt
产品活性：AVE 0991 sodium salt 是一种有效的非肽Ang-(1-7) 受体 Mas 激动剂。AVE 0991 sodium salt 与 [125I]-Ang-(1-7) 竞争性地结合到牛主动脉内皮细胞膜，IC50 为 21 nM。
研究领域：GPCR/G Protein
作用靶点：Angiotensin Receptor
In Vitro: AVE 0991 is a nonpeptide compound that evokes effects similar to Ang-(1-7) on the endothelium. AVE 0991 and unlabeled Ang-(1-7) compete for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50s of 21±35 and 220±280 nM, respectively. Peak concentrations of NO and O2- release by AVE 0991 sodium salt and Ang-(1-7) (both 10 μM) are not significantly different (NO: 295±20 and 270±25 nM; O2-: 18±2 and 20±4 nM). However, the released amount of bioactive NO is ≈5 times higher for AVE 0991 in comparison to Ang-(1-7).
In Vivo: AVE 0991 (0.58 nmol/g) produces a significant decrease of water diuresis in WT mice compared with vehicle-treated animals (0.06±0.03 mL versus 0.27±0.05; n=9 for each group; P<0.01). The antidiuretic effect of AVE 0991 (AVE) is associated with an increase in urine osmolality (1669±231.0 mOsm/KgH2O versus 681.1±165.8 mOsm/KgH2O in vehicle-treated mice; P<0.01). The genetic deletion of Mas abolishes the antidiuretic effect of AVE 0991 during water loading (0.37±0.10 mL [n=9] versus 0.27±0.03 mL [n=11] in AVE 0991-treated mice). As observed with C57BL/6 mice, administration of AVE 0991 (0.58 nmol/g) in water-loaded Swiss mice also produces a significant decrease of the urinary volume compared with vehicle-treated animals (0.13±0.05 mL [n=16] versus 0.51±0.04 mL [n=40]; P<0.01). One week of treatment with AVE-0991 produces a significant decrease in perfusion pressure (56.55±0.86 vs. 68.73±0.69 mmHg in vehicle-treated rats) and an increase in systolic tension (11.40±0.05 vs. 9.84±0.15 g in vehicle-treated rats), rate of tension rise (+dT/dt; 184.30±0.50 vs. 155.20±1.97 g/s in vehicle-treated rats), rate of tension fall (−dT/dt; 179.60±1.39 vs. 150.80±2.42 g/s in vehicle-treated rats). A slight increase in heart rate (HR) is also observed (220.40±0.71 vs. 214.20±0.74 beats/min in vehicle-treated rats.
相关产品：Covalent Screening Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Covalent Screening Library | Anti-Cardiovascular Disease Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Neurotransmitter Receptor Compound Library | Angiogenesis-Related Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Irbesartan hydrochloride | Dehydro Olmesartan | Losartan Carboxylic Acid | A81988 | Eprosartan | Angiotensin III, human, mouse TFA | (Sar1,Ile4,8)-Angiotensin II | Losartan-d3 Carboxylic Acid | Irbesartan-d4 | Saralasin acetate hydrate | Allisartan isoproxil | TRV-120027 | Mepixetil | Losartan carboxylic acid-d4 hydrochloride | Angiotensin amide | Sparsentan | YS-49 | Azilsartan medoxomil monopotassium | Angiotensin II human TFA | Angiotensin II (3-8), human TFA | [Sar1, Ile8]-Angiotensin II TFA | Tranilast sodium | SL910102 | Candesartan Cilexetil | L162389 | L-159282 | CGP48369 | Elisartan | Pratosartan | Novokinin
热门产品线：重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-15778A
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
• 50,000 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；
• 产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
• 提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
• 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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。
