血管緊張素Ⅱ作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetAngiotensin II humanCat. No.: HY-13948CAS No.: 4474-91-3分式: CHNO分量: 1046.18Sequence: Asp-Arg-Val-Tyr-Ile-His-Pro-PheSequence Shortening: DRVYIHPF作靶點(diǎn): Angiotensin Receptor; Apoptosis作通路: GPCR/G Protein; Apoptosis儲存式: Protect from light, stored under nitrogenPowder -80C 2 years-20C 1

2、 yearIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 50 mg/mL (47.79 mM)DMSO : 16.67 mg/mL (15.93 mM; Need ultrasonic)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration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

3、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；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light, stored under nitrogen)。-80C 儲存時，請?jiān)?6 個內(nèi)使，-20C 儲存時，請?jiān)?1 個內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；

4、 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶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 solution此案可獲得 0.83 mg/mL (0.79 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50

5、 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 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 solution此案可獲得 0.83 mg/mL (0.79 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.83

6、 mg/mL (0.79 mM); Clear solution此案可獲得 0.83 mg/mL (0.79 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Angiotensin II human (Angiotensin II) 主 作于 AT1 受體的管收縮劑。Angiotensin II human 刺激交感神經(jīng)刺激 ，增加醛 酮的物合成和腎功能。Angiotensin II human 誘導(dǎo)管平滑肌細(xì)胞

7、的長，增加成纖維細(xì)胞中 I 型和 III 型膠原的合成，導(dǎo)致管壁和肌增厚以及纖維化。Angiotensin II human 還可誘導(dǎo)細(xì)胞凋亡 (apoptosis)。IC & 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 receptor contributes tothe regulation of blood pressure and renal functi

8、on1. Angiotensin II raises blood pressure (BP) by a number ofactions, the most important ones being vasoconstriction, sympathetic nervous stimulation, increased aldosteronebiosynthesis and renal actions. Other Angiotensin II actions include induction of growth, cell migration, and mitosis ofvascular

9、 smooth muscle cells, increased synthesis of collagen type I and III in fibroblasts, leading to thickening of thevascular wall and myocardium, and fibrosis. These actions are mediated by type 1 Ang II receptors (AT1)2. At thecellular level, responsiveness to Angiotensin II is conferred by the expres

10、sion of the two classes of angiotensinreceptors (AT1 and AT2). The effects of Angiotensin II to increase blood pressure are mediated by AT1 receptors3.體內(nèi)研究 To distinguish the AT1 receptor population that is critical for the pathogenesis of hypertension, osmotic minipumps are implanted s.c. into each

11、 animal to infuse Angiotensin II (1,000 ng/kg/min) continuously for 4 weeks. Angiotensin II causes hypertension by activating AT1 receptors in the kidney promoting sodium reabsorption3.PROTOCOLAnimal Mice3Administration 3 (129C57BL/6) F1 mice lacking AT1A receptors for Angiotensin II are used. The m

12、ice are fed 10 gm/day gelled 0.25%NaCl diet that contains all nutrients and water. After 1 week of baseline collections, the animals are implanted withosmotic minipumps infusing Angiotensin II and are returned to the metabolic cage for 5 more days. Urinary sodiumcontent is determined by using an IL9

13、43 Automatic Flame photometer. After 28 days of Angiotensin II infusion,hearts are harvested, weighed, fixed in formalin, sectioned, and stained with Masson trichrome. All of the tissues areexamined by a pathologist (P.R.) without knowledge of genotypes.MCE has not independently confirmed the accura

14、cy of these methods. They are for reference only.Page 2 of 3 www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Oxid Med Cell Longev. 2019; 2019: 4025496. Oxid Med Cell Longev. 2019 Nov. J Cell Mol Med. 2020 Mar 12. J Cell Mol Med. 2019 Sep 11. Am J Physiol Cell Physiol. 2020 Mar 11.See more customer validations on HYPERLINK

15、www.MedChemE www.MedChemEREFERENCES1. de Gasparo 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 Hum Hypertens. 1995Nov;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 U S A. 2006 Nov21;103