(D-Pro⁷)-Angiotensin I/II (1-7)
目录号 : GA20155
(D-Pro⁷)-Angiotensin I/II (1-7) 是一种Mas受体拮抗肽，通过将Angiotensin-(1-7) 的C端Pro⁷替换为D-型脯氨酸而设计。
Cas No.:586962-44-9
Sample solution is provided at 25 µL, 10mM.
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(D-Pro⁷)-Angiotensin I/II (1-7) is a peptide antagonist of the Mas receptor, engineered by replacing the C-terminal Pro⁷ of Angiotensin-(1-7) with a D-proline[1]. The Mas receptor, a G-protein-coupled receptor for Ang-(1-7), elicits vasodilatory, anti-proliferative and anti-fibrotic protective signals upon activation[2]. (D-Pro⁷)-Angiotensin I/II (1-7) competitively blocks the binding of Angiotensin-(1-7) to Mas and is widely used to selectively interrupt ACE2/Ang-(1-7)/Mas-axis signaling in research[3].
In vitro, pretreatment of human pulmonary microvascular endothelial cells (PMVEC) with 100nM (D-Pro⁷)-Angiotensin I/II (1-7)(30min) completely abolished the protective effect of Ang-(1-7) against thrombin induced barrier disruption, reducing the trans-endothelial electrical resistance (TEER)[4]. In rat aortic vascular smooth muscle cells (VSMC) cultured in high glucose (25mM), 72h co-incubation with 1μM (D-Pro⁷)-Angiotensin I/II (1-7) reversed the inhibitory effect of Ang-(1-7) on high glucose-induced ErbB2 phosphorylation, restoring the p-ErbB2/t-ErbB2 ratio[5].
In vivo, (D-Pro⁷)-Angiotensin I/II (1-7) (10μM; 20min pre-incubation in isolated organ bath) reduced the maximal vasorelaxation evoked by Ang-(1-7) in rat renal arteries, completely blocking Ang-(1-7)-induced vasodilation and abolishing Ang-(1-7)-mediated activation of the NO-sGC-cGMP pathway[6]. (D-Pro⁷)-Angiotensin I/II (1-7) (0.1μM; 20min pre-incubation; vascular-bath perfusion) blocks an A-779-insensitive novel Ang-(1–7) receptor subtype and completely reverses the endothelium-dependent relaxation induced by Ang-(1–7) in isolated thoracic aortic rings from Sprague–Dawley rats[7].
References:
[1] Santos RA, Haibara AS, Campagnole-Santos MJ, et al. Characterization of a new selective antagonist for angiotensin-(1-7), D-pro7-angiotensin-(1-7). Hypertension. 2003;41(3 Pt 2):737-743.
[2] Santos RAS, Sampaio WO, Alzamora AC, et al. The ACE2/Angiotensin-(1-7)/MAS Axis of the Renin-Angiotensin System: Focus on Angiotensin-(1-7). Physiol Rev. 2018;98(1):505-553.
[3] Santos RA, Frézard F, Ferreira AJ. Angiotensin-(1-7): blood, heart, and blood vessels. Curr Med Chem Cardiovasc Hematol Agents. 2005;3(4):383-391.
[4] Klein N, Gembardt F, Supé S, et al. Angiotensin-(1-7) protects from experimental acute lung injury. Crit Care Med. 2013;41(11):e334-e343.
[5] Akhtar S, Chandrasekhar B, Attur S, Dhaunsi GS, Yousif MH, Benter IF. Transactivation of ErbB Family of Receptor Tyrosine Kinases Is Inhibited by Angiotensin-(1-7) via Its Mas Receptor. PLoS One. 2015;10(11):e0141657.
[6] Yousif MHM, Benter IF, Diz DI, Chappell MC. Angiotensin-(1-7)-dependent vasorelaxation of the renal artery exhibits unique angiotensin and bradykinin receptor selectivity. Peptides. 2017;90:10-16.
[7] Silva DM, Vianna HR, Cortes SF, Campagnole-Santos MJ, Santos RA, Lemos VS. Evidence for a new angiotensin-(1-7) receptor subtype in the aorta of Sprague-Dawley rats. Peptides. 2007;28(3):702-707.
(D-Pro⁷)-Angiotensin I/II (1-7) 是一种Mas受体拮抗肽，通过将Angiotensin-(1-7) 的C端Pro⁷替换为D-型脯氨酸而设计[1]。Mas受体是 Ang-(1-7) 的G蛋白偶联受体，激活后可产生扩血管、抗增殖和抗纤维化的保护性信号[2]。(D-Pro⁷)-Angiotensin I/II (1-7) 竞争性阻断 Angiotensin-(1-7) 与Mas的结合，被广泛用于选择性阻断ACE2/Ang-(1-7)/Mas轴信号传导研究[3]。
在体外，100nM (D-Pro⁷)-Angiotensin I/II (1-7) 预处理人肺微血管内皮细胞（PMVEC）30分钟，可完全消除 Ang-(1-7) 对凝血酶诱导的屏障破坏的保护作用，使跨内皮电阻（TEER）降低[4]。在25mM高糖培养的大鼠主动脉血管平滑肌细胞（VSMC）中，与1μM (D-Pro⁷)-Angiotensin I/II (1-7) 共孵育72小时，可逆转 Ang-(1-7) 对高糖诱导的ErbB2磷酸化的抑制作用，恢复p-ErbB2/t-ErbB2比值[5]。
在体内，(D-Pro⁷)-Angiotensin I/II (1-7)（10μM；离体器官浴中预孵育20分钟）可减弱Ang-(1-7) 在大鼠肾动脉中诱导的最大舒张反应，完全阻断Ang-(1-7) 的血管舒张作用，并消除Ang-(1-7) 介导的NO-sGC-cGMP通路激活[6]。(D-Pro⁷)-Angiotensin I/II (1-7)（0.1μM；20分钟预孵育；血管浴灌注）可阻断一种对A-779不敏感的新型Ang-(1–7) 受体亚型，并完全逆转Ang-(1–7) 在Sprague–Dawley大鼠离体胸主动脉环中诱导的内皮依赖性舒张反应[7]。
| Cell experiment [1]: | |
Cell lines | Human pulmonary microvascular endothelial cells |
Preparation Method | Human pulmonary microvascular endothelial cells (PMVECs, passages 4–8) were grown to confluence in polycarbonate wells containing gelatin-coated gold microelectrodes. Following a 30 minute recording of baseline resistance, the Ang-(1–7) receptor blocker (D-Pro⁷)-Angiotensin I/II (1-7)(100nM), the bradykinin receptor blocker icatibant (1µM), the NO synthase inhibitor Nω-nitro-L-arginine methyl ester (l-NAME; 1mM), or respective vehicle controls were added, followed after 15 minutes by Ang-(1–7) (100nM) or vehicle and after an additional 30 minutes by thrombin (0.2U/mL). Transendothelial electrical resistance (TEER) measurements were performed using an electrical cell substrate impedance sensing system. TEER values were recorded continuously up to 75 minutes after thrombin stimulation. |
Reaction Conditions | 100nM; 30min |
Applications | Pretreatment of human pulmonary microvascular endothelial cells (PMVEC) with (D-Pro⁷)-Angiotensin I/II (1-7) completely abolished the protective effect of Ang-(1-7) against thrombin induced barrier disruption, reducing the trans-endothelial electrical resistance (TEER). |
| Animal experiment [2]: | |
Animal models | Sprague–Dawley rats |
Preparation Method | 7–9-month-old male Hanover Sprague–Dawley rats were maintained in collective cages in an appropriate room with controlled temperature and with a 12h light cycle. The vasorelaxant activity of Ang-(1–7) was measured in vessels with or without functional endothelium pre-contracted to the same tension level (approximately 1.5g of tension) with submaximal concentrations of phenylephrine (0.03–0.1μM). Ang-(1–7) was added in increasing cumulative concentrations once the response to phenylephrine had stabilized. In an attempt to determine which receptor is involved in the vasorelaxant effect of Ang-(1–7), experiments were performed in endothelium-containing vessels, in the presence of the Ang-(1–7) antagonists A-779 (0.1, 1.0 or 10μM) or (D-Pro⁷)-Angiotensin I/II (1-7) (0.1μM); the B2 receptor antagonist HOE 140 (1μM), the Ang II receptor antagonists CV11974 (0.01μM; AT1 antagonist) or PD123319 (1μM; AT2 antagonist). As a control, another vessel segment from each rat was simultaneously monitored for Ang-(1–7) effects alone. |
Dosage form | 0.1μM; 20min pre-incubation, vascular-bath perfusion |
Applications | (D-Pro⁷)-Angiotensin I/II (1-7) blocks an A-779-insensitive novel Ang-(1–7) receptor subtype and completely reverses the endothelium-dependent relaxation induced by Ang-(1–7) in isolated thoracic aortic rings from Sprague–Dawley rats. |
References: | |
| Cas No. | 586962-44-9 | SDF | |
| 分子式 | C41H62N12O11 | 分子量 | 899.02 |
| 溶解度 | 1 mg/mL in Water | 储存条件 | Store at -20°C |
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| 1 mM | 1.1123 mL | 5.5616 mL | 11.1232 mL |
| 5 mM | 0.2225 mL | 1.1123 mL | 2.2246 mL |
| 10 mM | 0.1112 mL | 0.5562 mL | 1.1123 mL |
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- Purity: 98.68%
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