Endothelin-2, human
(Synonyms: 内皮素2,Endothelin-2 (human, canine); Human endothelin-2) 目录号 : GC35987
A peptide vasoconstrictor
Cas No.:123562-20-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[1]For the assay of pressor activity, male Wistar rats weighing 300-350 g are anesthetized with urethane (1 g/kg i.p.) and pretreated with atropine (0.25 mg/kg i.v.), propranolol (1 mg/kg i.v.), and bunazocine (1 mg/kg i.v.). Additional maintenance doses (one-half of the initial doses) of the autonomic blockades are administered every 3-4 hr. Each animal is given only one bolus of Endothelin-2. 1 nM of Endothelin-2 in 50 μL of buffer is bolus injected from a cannula inserted in the right femoral vein. The blood pressure is recorded from a cannula, which is placed in the right carotid artery and connected to a pressure transducer[1]. |
References: [1]. Grimshaw MJ, et al. Endothelin-2 is a macrophage chemoattractant: implications for macrophage distribution in tumors. Eur J Immunol. 2002 Sep;32(9):2393-400. | |
Endothelin-2 is a peptide vasoconstrictor and ligand for the endothelin (ET) receptors ETA and ETB (Kbs= 32.8 and 1.33 nM, respectively).1 It induces β-arrestin recruitment in CHO-K1 cells expressing human ETA and ETB (pD2s =8.75 and 8.55, respectively). Ex vivo, endothelin-2 induces vformal asoconstriction in isolated rat mesenteric arterial beds (ED50 = 90.8 pmol).2 Endothelin-2 also induces contraction of isolated rat uteri, an effect which is reversed by the ETA antagonist BQ-123 but not the ETB antagonist BQ-788 .3 Infusion of endothelin-2 restores vasoconstriction of vessels at the follicular apex of the ovarian follicle and ovulation in Amhr2cre/+Smo2 mice.4
1.Maguire, J.J., Kuc, R.E., Pell, V.R., et al.Comparison of human ETA and ETB receptor signalling via G-protein and β-arrestin pathwaysLife Sci.91(13-14)544-549(2012) 2.Douglas, S.A., and Hiley, C.R.Endothelium-dependent vascular activities of endothelin-like peptides in the isolated superior mesenteric arterial bed of the ratBr. J. Pharmacol.101(1)81-88(1990) 3.Kousides, M., Story, M.E., and Pennefather, J.N.Endopeptidase 24.11 inhibition does not modify uterotonic effects of endothelins in rat uterusPeptides19(9)1585-1593(1998) 4.Migone, F.F., Cowan, R.G., Williams, R.M., et al.In vivo imaging reveals an essential role of vasoconstriction in rupture of the ovarian follicle at ovulationProc. Natl. Acad. Sci. USA113(8)2294-2299(2016)
| Cas No. | 123562-20-9 | SDF | |
| 别名 | 内皮素2,Endothelin-2 (human, canine); Human endothelin-2 | ||
| 分子式 | C115H160N26O32S4 | 分子量 | 2546.92 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.3926 mL | 1.9632 mL | 3.9263 mL |
| 5 mM | 0.0785 mL | 0.3926 mL | 0.7853 mL |
| 10 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL |
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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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The loss of Endothelin-2 exhibits an anticancer effect in A549 human lung adenocarcinoma cell line
Can J Physiol Pharmacol 2022 Aug 1;100(8):818-827.PMID:35679618DOI:10.1139/cjpp-2022-0006.
Lung cancer is the leading cause of cancer-related deaths worldwide, and adenocarcinoma is the most common subtype of lung cancer. Endothelin-2 (ET-2) is expressed in the epithelium of alveoli, and its expression is increased in cancer. However, the role of ET-2 in lung adenocarcinoma remains unclear. This study aimed to investigate the pathophysiological functions of ET-2 in A549 human lung adenocarcinoma cells. We analyzed the expression of ET-2 mRNA in lung adenocarcinoma tissues compared with that in nontumor lung tissues using public online databases. The function of ET-2 in A549 cells was investigated using siRNA. ET-2 mRNA level was upregulated in lung adenocarcinoma tissues, and high ET-2 level was associated with poor overall survival in patients with lung adenocarcinoma. ET-2 silencing reduced the proliferation, migration, and invasion, and enhanced apoptosis in A549 cells. Mechanistically, ET-2 silencing reduced the expression levels of X-linked inhibitor of apoptosis and survivin, which are members of the inhibitor apoptosis protein family. In addition, silencing ET-2 inhibited epithelial-mesenchymal transition, which halted migration. Therefore, the specific targeting of ET-2 may be a potential treatment strategy for lung adenocarcinoma.
Endothelin 2: a key player in ovulation and fertility
Reproduction 2022 Mar 5;163(4):R71-R80.PMID:35167488DOI:10.1530/REP-21-0313.
Ovulation is the fundamental biological process during which an oocyte is expelled from the ovary, and it is an essential step toward establishing a pregnancy. Understanding regulatory mechanisms governing the ovulation process is essential for diagnosing and treating causes of infertility, identifying contraceptive targets, and developing novel contraception methods. Endothelin-2 (EDN2) is a 21 amino acid-long peptide that is transiently synthesized by granulosa cells of the ovulatory follicle prior to ovulation and plays an essential role in ovulation via promoting contraction in the myofibroblast cells of the theca layer of the follicle. This review describes the organization of the endothelin system, summarizes recent findings on the expression and synthesis of the endothelin system in the ovary, illustrates the roles that EDN2 plays in regulating ovulation, and discusses EDN2 as a potential target of contraception.
Disulfide-Driven Cyclic Peptide Synthesis of Human Endothelin-2 with a Solid-Supported Npys-Cl
J Org Chem 2020 Feb 7;85(3):1495-1503.PMID:31793782DOI:10.1021/acs.joc.9b02362.
We report here the synthesis of human Endothelin-2, a peptide of 21 amino acid residues with two disulfide bonds, based on the novel idea of a disulfide-driven cyclic peptide synthesis (DdCPS). This synthesis has two steps: (1) a one-pot solid-phase disulfide ligation of two different sulfur-containing peptide fragments using an Npys-Cl resin and (2) intramolecular cyclization of the disulfide peptide via amide bond formation using a thioester ligation. Human Endothelin-2 was obtained in a total yield of 2.2% with two such DdCPS procedures and subsequent deprotection and HPLC purification. This strategy is the basis of a new solid-phase assisted practical synthesis of cyclic disulfide peptides.
Sirtuin-1 inhibits Endothelin-2 expression in human granulosa-lutein cells via hypoxia inducible factor 1 alpha and epigenetic modifications†
Biol Reprod 2021 Feb 11;104(2):387-398.PMID:33112382DOI:10.1093/biolre/ioaa199.
Endothelin-2 (EDN2) expression in granulosa cells was previously shown to be highly dependent on the hypoxic mediator, hypoxia inducible factor 1 alpha (HIF1A). Here, we investigated whether sirtuin-1 (SIRT1), by deacetylating HIF1A and class III histones, modulates EDN2 in human granulosa-lutein cells (hGLCs). We found that HIF1A was markedly suppressed in the presence of resveratrol or a specific SIRT1 activator, SRT2104. In turn, hypoxia reduced SIRT1 levels, implying a mutually inhibitory interaction between hypoxia (HIF1A) and SIRT1. Consistent with reduced HIF1A transcriptional activity, SIRT1 activators, resveratrol, SRT2104, and metformin, each acting via different mechanisms, significantly inhibited EDN2. In support, knockdown of SIRT1 with siRNA markedly elevated EDN2, whereas adding SRT2104 to SIRT1-silenced cells abolished the stimulatory effect of siSIRT1 on EDN2 levels further demonstrating that EDN2 is negatively correlated with SIRT1. Next, we investigated whether SIRT1 can also mediate the repression of the EDN2 promoter via histone modification. Chromatin immunoprecipitation (ChIP) analysis revealed that SIRT1 is indeed bound to the EDN2 promoter and that elevated SIRT1 induced a 40% decrease in the acetylation of histone H3, suggesting that SIRT1 inhibits EDN2 promoter activity by inducing a repressive histone configuration. Importantly, SIRT1 activation, using SRT2104 or resveratrol, decreased the viable numbers of hGLC, and silencing SIRT1 enhanced hGLC viability. This effect may be mediated by reducing HIF1A and EDN2 levels, shown to promote cell survival. Taken together, these findings propose novel, physiologically relevant roles for SIRT1 in downregulating EDN2 and survival of hGLCs.
Identification of endothelin-1, Endothelin-2 and endothelin-3 in human endometrium
J Reprod Fertil 1993 May;98(1):251-5.PMID:8345469DOI:10.1530/jrf.0.0980251.
This study determined the presence of specific endothelin isoforms in human endometrium using high performance liquid chromatography (HPLC) combined with radioimmunoassay, and immunocytochemistry to detect the endothelin precursors (proendothelin-1, proendothelin-2 and proendothelin-3). Endothelin-like immunoreactivity was measured in HPLC eluates using antisera raised in rabbits against the carboxy-terminal heptapeptide of endothelin-1, which is common to the three endothelin isoforms. Of eight endometrial samples analysed by HPLC, three were in the proliferative phase of the cycle, and five in the secretory phase. Endothelin-1 was detected in seven samples, whereas Endothelin-2 and endothelin-3 were seen in four and five specimens, respectively. No relationship was seen between endothelin isoforms and the stage of the cycle. Immunocytochemistry was performed on five proliferative and three secretory phase tissues. When present, staining for the precursor proendothelins was localized to endometrial glandular and luminal epithelium (proendothelin-1, 5 of 8; proendothelin-2, 5 of 8; proendothelin-3, 6 of 8). In two sections, staining was also seen in vascular endothelium using antibody raised against proendothelin-1 (n = 1) and proendothelin-3 (n = 1). These data provide evidence that the three endothelin isoforms are present in human endometrium, and suggest that these potent vasoactive agents may play a role in the paracrine control of the uterine vascular bed.