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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAngiotensin II humanCat. No.: HY-13948CAS No.: 4474-91-3Synonyms: Angiotensin II; Hypertensin II; Ang II; DRVYIHPF分式: CHNO分量: 1046.18Sequence: Asp-Arg-Val-Tyr-Ile-His-Pro-PheSequence Shortening: DRVYIHPF作靶点: Angiotensin Receptor
2、作通路: GPCR/G Protein储存式: Protect from light, stored under nitrogenPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 该产品在溶液状态不稳定,建议您现现配,即刻使。溶解性数据体外实验 H2O : 50 mg/mL (47.79 mM)DMSO : 16.67 mg/mL (15.93 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 1
3、0 mg Concentration制备储备液1 mM 0.9559 mL 4.7793 mL 9.5586 mL5 mM 0.1912 mL 0.9559 mL 1.9117 mL10 mM 0.0956 mL 0.4779 mL 0.9559 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄
4、清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (0.79 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (0.79 mM); Clear solution3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 0.83 m
5、g/mL (0.79 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Angiotensin II human作于 AT1 和 AT2 受体的管收缩剂。IC50 & Target Angiotensin receptor (AT receptor) 1体外研究 Most of the known actions of Angiotensin II (Ang II) are mediated by AT1 receptors, the AT2 receptorcontributes to the regulation of blood pressure and
6、 renal function 1. Angiotensin II raises blood pressure(BP) by a number of actions, the most important ones being vasoconstriction, sympathetic nervousstimulation, increased aldosterone biosynthesis and renal actions. Other Angiotensin II actions includeinduction of growth, cell migration, and mitos
7、is of vascular smooth muscle cells, increased synthesis ofcollagen type I and III in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis.These actions are mediated by type 1 Ang II receptors (AT1) 2. At the cellular level, responsiveness toAngiotensin II is conferred
8、 by the expression of the two classes of angiotensin receptors (AT1 and AT2). Theeffects of Angiotensin II to increase blood pressure are mediated by AT1 receptors 3.体内研究 To distinguish the AT1 receptor population that is critical for the pathogenesis of hypertension, osmoticminipumps are implanted
9、s.c. into each animal to infuse Angiotensin II (1,000 ng/kg/min) continuously for 4weeks. Angiotensin II causes hypertension by activating AT1 receptors in the kidney promoting sodiumreabsorption 3.PROTOCOLAnimal Mice 3Administration 3 (129C57BL/6) F1 mice lacking AT1A receptors for Angiotensin II a
10、re used. The mice are fed 10 gm/daygelled 0.25% NaCl diet that contains all nutrients and water. After 1 week of baseline collections, the animalsare implanted with osmotic minipumps infusing Angiotensin II and are returned to the metabolic cage for 5more days. Urinary sodium content is determined b
11、y using an IL943 Automatic Flame photometer. After 28days of Angiotensin II infusion, hearts are harvested, weighed, fixed in formalin, sectioned, and stained withMasson trichrome. All of the tissues are examined by a pathologist (P.R.) without knowledge of genotypes.MCE has not independently confir
12、med the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE户使本产品发表的科研献 Am J Physiol Heart Circ Physiol. 2018 Mar 1;314(3):H580-H592. Nephrology (Carlton). 2018 Oct 8.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. de Gasparo
13、M, et al. International union of pharmacology. XXIII. The angiotensin II receptors. Pharmacol Rev. 2000 Sep;52(3):415-72.2. Fyhrquist F, et al. Role of angiotensin II in blood pressure regulation and in the pathophysiology of cardiovascular disorders. J HumHypertens. 1995 Nov;9 Suppl 5:S19-24.3. Crowley SD, et al. Angiotensin II causes hypertension and cardiac hypertrophy through its receptors in the kidney. Proc Natl Acad Sci US A. 2006 Nov 21;103(47):17985-90
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