Angiotensin I (human, mouse, rat)
(Synonyms: 血管紧张素 1 (人)) 目录号 : GP10087血管紧张素 I(人、小鼠、大鼠)是血管收缩肽血管紧张素 II 的前体,被血管紧张素转换酶 (ACE) 裂解。
Cas No.:484-42-4
Sample solution is provided at 25 µL, 10mM.
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Angiotensin I (Ang I) (C62H89N17O14), with the sequence H-Asp-Arg-Val-Tyr-Ile-His-Pro-Phe-His-Leu-OH, is formed by the action of renin on angiotensinogen. Renin is produced in the kidneys in response to renal sympathetic activity, decreased intrarenal blood pressure (<90mmHg systolic blood pressure) at the juxtaglomerular cells. Ang I appears to have no biological activity and exists solely as a precursor to angiotensin II (A II). Ang I is cleaved to Ang II by the angiotensin-converting enzyme (ACE). Ang II increases blood pressure by stimulating the Gq protein in vascular smooth muscle cells (which in turn activates contraction by an IP3-dependent mechanism).
References:
1. Lundequist, A. et al. J. Biol. Chem. 279, 32339 (2004); Olson, S. et al. Am. J. Physiol. Lung. Cell Mol. Physiol. 287, L559 (2004); Sanker, S. et al. J. Biol. Chem. 272, 2963 (1997).
2. Preston RA, Materson BJ, Reda DJ, et al. Age-Race Subgroup Compared With Renin Profile as Predictors of Blood Pressure Response to Antihypertensive Therapy. JAMA. 1998;280(13):1168-1172. doi:10.1001/jama.280.13.1168.
Cas No. | 484-42-4 | SDF | |
别名 | 血管紧张素 1 (人) | ||
化学名 | Angiotensin I (human, mouse, rat) | ||
Canonical SMILES | CCC(C)C(C(=O)NC(CC1=CN=CN1)C(=O)N2CCCC2C(=O)NC(CC3=CC=CC=C3)C(=O)NC(CC4=CN=CN4)C(=O)NC(CC(C)C)C(=O)O)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(C(C)C)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC(=O)O)N | ||
分子式 | C62H89N17O14 | 分子量 | 1296.5 |
溶解度 | ≥ 129.6mg/mL in DMSO, ≥ 124.2 mg/mL in Water | 储存条件 | Desiccate at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 0.7713 mL | 3.8565 mL | 7.7131 mL |
5 mM | 0.1543 mL | 0.7713 mL | 1.5426 mL |
10 mM | 0.0771 mL | 0.3857 mL | 0.7713 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Potency and selectivity of RXP407 on human, rat, and mouse angiotensin-converting enzyme
By screening phosphinic peptide libraries, we recently reported the discovery of RXP407 (Ac-Asp-PheY(PO2-CH2)LAla-Ala-NH2), a potent N-domain-selective inhibitor of recombinant human angiotensin-converting enzyme (ACE). Preliminary studies to evaluate the in vivo activity of RXP407 in rat led us to suspect possible differences in the binding property of RXP407 between human and rat ACE. The aim of the present study was thus to determine the potency of RXP407 toward rat and mouse ACEs, as compared to non-recombinant human ACE, and to assess the efficacy of this inhibitor in discriminating between the N- and C-domains of these ACE enzymes. By comparing the ability of RXP407 to block purified somatic and germinal ACE from mice, RXP407 was shown to be a potent N-domain-selective inhibitor of mouse somatic ACE, a behavior similar to that observed with human somatic ACE. In contrast, RXP407 appeared less potent toward purified ACE from rat and furthermore was unable to block ACE activity present in crude rat plasma. This study demonstrated that for further evaluation of the in vivo efficacy of RXP407, mice rather than rats should be used as the animal model. Thus, following the change in the Ac-S-D-K-P plasmatic levels, after i.v. injection of RXP407 to mice, will permit the potency and selectivity of this novel ACE inhibitor to be assessed.
Analysis of the evolution of angiotensin II type 1 receptor gene in mammals (mouse, rat, bovine and human)
The nucleotide and amino acid sequences for mouse angiotensin II (AII) type 1A and 1B receptors were deduced from their complementary and genomic DNAs. Evolutionary analyses based on the nucleotide sequences of the coding region of AII type 1 receptor genes indicated that the duplication event of the type 1 gene occurred 24 +/- 2 million years ago before the divergence between the rat and mouse but after the divergence between rodents and the human/artiodactyls couple. This conclusion was consistent with the results of genomic Southern blot analyses, which revealed that the mouse and rat possess 2 similar but separate genes, whereas the bovine and human have only a single class gene.