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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作靶點: Angiotensin Receptor
2、作通路: GPCR/G Protein儲存式: Protect from light, stored under nitrogenPowder -80C 2 years-20C 1 yearIn solvent -80C 6 months-20C 1 month* 該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)現(xiàn)配,即刻使。溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度,選擇合適的溶劑配制儲備液,并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?,再依次添加助溶?/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE(為保證實驗結(jié)果的可靠性,體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當天使;澄
4、清的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (0.79 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (0.79 mM); Clear solution3. 請依序添加每種溶劑: 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 受體的管收縮劑。IC50 & Target Angiotensin receptor (AT receptor) 1體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻 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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