血管緊張素 (1-7)作用機制 - Medchemexpress - MCE中國

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作靶點: Angiotensin Receptor; Angiotensin-converting Enzyme (ACE)作通路: GPCR/G Protein; Metabolic Enzyme/Protease儲存式: Powder -80C 2 years-20C 1 yearIn so

2、lvent -80C 6 months-20C 1 month溶解性數據體外實驗 H2O : 30.2 mg/mL (33.59 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液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請根據產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

3、凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。BIOLOGICAL ACTIVITY物活性 Angiotensin 1-7 (Ang-(1-7) 腎素-管緊張素系統(tǒng) (RAS) 的主 活性成分，由管緊張素轉換酶 2 (ACE2) 分解管 緊張素 II 產。Angiotensin 1-7 抑制純化的管緊張素轉換酶 (ACE) 活性，IC50 值為 0.65 M。Angiotensin 1-7 通過抑制管緊張素轉換酶和釋放氧化氮，可作為激肽誘導的管舒張的局部協(xié)同調節(jié)劑。A

4、ngiotensin 1-7 阻斷 AngII 誘導的平滑肌細胞增殖和肥，并顯對內的抗管成和長抑制作。Angiotensin 1-7 顯出抗炎活性12 3。IC & Target IC50: 0.65 M (ACE)2Page 1 of 2 www.MedChemE體外研究 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.體內研究 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.戶使本產品發(fā)表的科研獻

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