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。

A81988

CAS No. : 141887-34-5

MCE 站：A81988

产品活性：A81988 是一种有效的竞争性的非肽类的血管紧张素 AT₁ 受体拮抗剂。

研究领域：GPCR/G Protein

作用靶点：Angiotensin Receptor

In Vitro: A81988 (A-81988) is labeled with tritium to high specific activity (16 Ci/mmol) and radioligand binding assays performed in rat liver membranes. [³H]A81988 binds with high affinity (K_D=0.57 nM) and the K_D determined from kinetics assays is similar. Non-specific binding (defined with 1 μM angiotensin-II) is very low (< 6% at the K_D). The binding of [³H]A81988 is competitive and exhibits appropriate pharmacological specificity for compounds acting at angiotensin AT₁ receptors.

In Vivo: To verify this hypothesis, B₂^-/- or wild-type mice (B₂^+/+) are administered a nonpeptide antagonist of Ang II type 1 (AT₁) receptors (A81988) from conception through 180 days of age. Untreated B₂^+/+ and B₂^-/- served as controls. Blood pressure (BP) and heart rate are monitored with the use of tail-cuff plethysmography at regular intervals. Ventricular weights, diameters, wall thickness, chamber volume, and myocardial fibrosis are measured at 40 and 180 days. No differences are observed in BP, heart rate, and cardiac weight and dimensions between treated and untreated B₂^+/+. The BP of AT₁ antagonist-treated B₂^-/- is reduced until 70 days; then, it increases to the levels found in untreated B₂^-/-. AT₁ receptor blockade results in a reduction in left ventricular mass, chamber volume, and wall thickness and abrogated myocardial fibrosis in B₂^-/-. A81988 (A-81988) decreases the BP of Bk2r^-/- either in normosodic conditions or after sodium deprivation, whereas in Bk2r^+/+ it produces a modest decrease under hyposodic conditions only.

相关产品：Angiotensin II human  |  Losartan  |  A 779  |  Telmisartan  |  PD 123319 ditrifluoroacetate  |  AVE 0991  |  Valsartan  |  Olmesartan  |  Tranilast  |  YS-49  |  Irbesartan  |  Candesartan  |  CGP-42112  |  Olodanrigan  |  Sparsentan  |  C-Type Natriuretic Peptide (CNP) (1-22), human  |  Azilsartan medoxomil  |  Angiotensin II 5-valine  |  Eprosartan mesylate  |  Angiotensin (1-7) (acetate)  |  Fimasartan  |  Tasosartan  |  Angiotensin II (3-8), human TFA

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。