血管紧张素 (1-7)作用机制 - Medchemexpress - MCE中国

1、Product Data SheetAngiotensin (1-7)Cat. No.: HY-12403CAS No.: 51833-78-4分式: CHNO分量: 899Sequence: Asp-Arg-Val-Tyr-Ile-His-ProSequence Shortening: DRVYIHP作靶点: Angiotensin Receptor; Angiotensin-converting Enzyme (ACE)作通路: GPCR/G Protein; Metabolic Enzyme/Protease储存式: Powder -80C 2 years-20C 1 yearIn so

2、lvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 30.2 mg/mL (33.59 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.1123 mL 5.5617 mL 11.1235 mL5 mM 0.2225 mL 1.1123 mL 2.2247 mL10 mM 0.1112 mL 0.5562 mL 1.1123 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；旦配成溶液，请分装保存，避免反复

3、冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。BIOLOGICAL ACTIVITY物活性 Angiotensin 1-7 (Ang-(1-7) 肾素-管紧张素系统 (RAS) 的主 活性成分，由管紧张素转换酶 2 (ACE2) 分解管 紧张素 II 产。Angiotensin 1-7 抑制纯化的管紧张素转换酶 (ACE) 活性，IC50 值为 0.65 M。Angiotensin 1-7 通过抑制管紧张素转换酶和释放氧化氮，可作为激肽诱导的管舒张的局部协同调节剂。A

4、ngiotensin 1-7 阻断 AngII 诱导的平滑肌细胞增殖和肥，并显对内的抗管成和长抑制作。Angiotensin 1-7 显出抗炎活性12 3。IC & Target IC50: 0.65 M (ACE)2Page 1 of 2 www.MedChemE体外研究 Angiotensin 1-7 (Ang-(1-7) inhibits cultured vascular smooth muscle cell growth, whereas equal molar concentrationof Ang II stimulates cell growth2.Angiotensin 1-

5、7 (Ang 1-7) abrogates the methylglyoxal-modified albumin (MGA)-stimulated myofibroblastphenotype by inhibiting the chronic stimulation of the TGF-ERK pathway in NRK-52E cells4.体内研究 Daily Angiotensin 1-7 (Ang-(1-7) treatment (0.01-0.06 mg/kg) results in significant amelioration of DSS-inducedcolitis.

6、 Colitis-associated phosphorylation of p38, ERK1/2 and Akt is reduced by Ang 1-7 treatment3.PROTOCOLKinase Assay 1 Competition assays using purified canine ACE are determined using a fixed concentration of the substrate Hip-His-Leu (1 mM) and varying the concentrations of the competing agents Lisino

7、pril (0.1 to 100 nM), Angiotensin (1-7) (10nM to 10 M), or Sar1, Thr8-Ang II (10 nM to 10 M). Inhibitory constants (IC50) are determined from the respectivecompetition curves. To study the effect of Angiotensin (1-7) on BK metabolism in intact coronary rings, 125I-Tyr0-BK(final concentration of 1 nM

8、) is added to the tubes containing three rings preincubated with 1 mL Krebs buffer andaerated with 95% O2 and 5% CO2 at 37C. Lisinopril (2 M), Angiotensin (1-7) (2 M), or Krebs buffer as control areadded to the rings 10 minutes before addition of the radiolabeled BK. Aliquots of the incubation mediu

9、m areremoved at 5, 10, and 20 minutes and diluted with 1% HFBA to inhibit peptidase activity1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 2 500 M Methylglyoxal is incubated with 100 M BSA dissolved in phosphate buffered saline (PBS) for 2

10、4 hours, thenwashed on 10 kDa filters to remove excess methyl glyoxal, reconstituted with DMEM/F12 serum free media andpassed through a 0.2 micron filter. TGF- (5 ng/mL) is prepared to treat cells in a subset of experiments. Cells areco-treated with one or combinations of the following: Angiotensin

11、(1-7) (100 nM), D-Ala7-Ang-(1-7) (10 M), ERK1/2kinase inhibitor, PD 98059 (1 M), TGF- receptor kinase inhibitor; SB525334 (1 M), the AT1 receptor antagonistLosartan (1 M), the renin inhibitor Aliskerin (1 M) and the ACE inhibitor Lisinopril (1 M)2.MCE has not independently confirmed the accuracy of

12、these methods. They are for reference only.Animal Mice3Administration 34 Male and female BALB/c mice (1:1 ratio, 6-10 weeks old, mean weight 20 g.) are used. Angiotensin fragment 1-7acetate salt hydrate (Ang 1-7) is dissolved in 0.9% saline (vehicle) at 1 mg/mL and stored at -80C. Various doses(0.01

13、, 0.06, 0.1, 0.3 and 1 mg/kg) are freshly prepared from the stock each day of the experiment, and administeredto mice by daily intra-peritoneal (i.p) injections in a volume of 500 L per injection, either before (prophylacticapproach) or after (treatment approach) DSS treatment. A779 (MAS-1 R antagon

14、ist) is similarly dissolved in distilledwater at 1 mg/mL and stored at -80C. A freshly prepared dose of 1 mg/kg is administered to a second group ofmice by daily i.p injections in a volume of 500 L daily (for 4 days) along with colitis induction (prophylacticapproach). A third group of mice receive

15、DSS containing water and daily i.p injections of 0.9% saline (vehicle). Thefourth group receive DSS containing water along with daily i.p injections with Dexamethasone (DEX) at doses of 0.01-1.0 mg/kg or its vehicle (0.9% saline) (prophylactic approach).Rats4Twenty six ovariectomized female Wistar r

16、ats weighing 20020 g are used. Angiotensin (1-7) is administeredintravenously by a microsyringe pump at two different continuous doses of 100 and 300 ng/kg/min afterantagonist/saline infusion. Each dose is infused for 15 min; and MAP, RPP, and RBF are recorded during Angiotensin(1-7) infusion and th

17、e last 3-5 min of each dose measured as “response to Angiotensin (1-7) infusion”. DuringAngiotensin (1-7) infusion, RPP is sustained at pre-Ang1-7 infusion levels via an adjustable aortic clamp.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献

18、Page 2 of 3 www.MedChemE Int J Clin Exp Med. 2019;12(5):4773-4780.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Vaz-Silva J, et al. The vasoactive peptide angiotensin-(1-7), its receptor Mas and the angiotensin-converting enzyme type 2 are expressed in the humanendometrium. Reprod Sci. 2009 Mar;16(3):247-56.2. Li P, et al. Angiotensin-(1-7) augments bradykinin-induced vasodilation by competing with ACE and releas