Endothelin 1 (human, porcine)

Cat. No. 1160 16 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Potent vasoconstrictor peptide

别名： ET-1

纯度： ≥95% (HPLC)

引用文献 (16)

生物活性 Scientific Data 技术数据溶解性计算器说明书参考文献

生物活性 for Endothelin 1 (human, porcine)

Endothelin 1 (human, porcine) is a potent endogenous peptide agonist at ET_A and ET_B receptors. Produces strong vasoconstriction and pressor responses. Competitive binding assay shows that Endothelin 1 reversibly binds to receptors (IC₅₀ values are 0.12 nM and 0.15 nM at ET_B and ET_A receptors respectively). Potency is dependent on blood vessel type (EC₅₀ ranges from 2.72 nM - 17.4 nM). Activates PLC (EC₅₀ = 0.3 nM), increases production of PGE₂ (EC₅₀ = 12 nM) and induces intracellular calcium release in human ciliary muscle cells. Also upregulates leptin mRNA expression and secretion in adipocytes (EC₅₀ = 8.8 nM).

Scientific Data

Multiplex Immunoassay

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Pluripotent stem cell-derived cardiomyocytes secrete Pro-BNP in response to small molecule-induction of cardiac hypertrophy Cardiomyocytes were treated with the vasoconstrictor, ET-1 (Endothelin-1; Catalog # 1160), or one of two L-type calcium channel inhibitors, Doxorubicin (Catalog # 2252) or Verapamil (Catalog # 0654). Levels of the cardiac hypertrophy marker, Pro-Brain Natriuretic Peptide (Pro-BNP), were detected via Luminex^® bead-based multiplex assay (Catalog # LXSAH). A substantial increase in Pro-BNP was detected in the medium of cardiomyocytes treated with ET-1, a known inducer of cardiac hypertrophy. Conversely, Doxorubicin and Verapamil decreased Pro-BNP secretion from cardiomyocytes.

ELISA

ET1 differentiated cardiomyocytes concentration dependent effect on Pro-ANP

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Differentiated cardiomyocytes respond physiologically to Endothelin-1 induced hypertrophy Cardiomyocytes differentiated from BG01V human embryonic stem cells were treated with Endothelin-1 (ET-1; Catalog # 1160) for 28 hours to induce cardiac hypertrophy. Levels of Pro-Atrial Natriuretic peptide (Pro-ANP) secretion, which is known to be elevated during cardiac hypertrophy, were assessed using ELISA (Catalog # DANP00). As expected, detection of Pro-ANP increased proportionally with the concentration of Endothelin-1 treatment.

Western Blot

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Endothelin Induces Expression of Atrial Natriuretic Peptide in Cardiomyocytes Derived from iPSCs JOY6 human iPSCs were differentiated into beating cardiomyocytes. After 21 days of differentiation cardiomyocytes were treated with 5 nM of Endothelin-1 (ET-1; Catalog # 1160) for 25.5 hours to induce cardiac hypertrophy. The level of secreted Pro-Atrial Natriuretic peptide (Pro-ANP), which is known to be elevated during cardiac hypertrophy, was assessed using (A) Western Blot and (B) ELISA (Human NTProANP Quantikine^® ELISA; Catalog # DANP00). As expected, detection of Pro-ANP was increased in Endothelin-1 treated cells.

技术数据 for Endothelin 1 (human, porcine)

分子量	2492
公式	C₁₀₉H₁₅₉O₃₂N₂₅S₅
序列	CSCSSLMDKECVYFCHLDIIW (Modifications: Disulfide bridges 1-15, 3-11)
储存	Store at -20°C
纯度	≥95% (HPLC)
CAS Number	117399-94-7
PubChem ID	16133807
InChI Key	ZUBDGKVDJUIMQQ-ZTNLKOGPSA-N
Smiles	[H][C@](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@]2([H])CSSC[C@]([H])(NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@H](CC2=CC=CC=C2)C(=O)N1)([C@@H](C)CC)C(=O)N[C@@]([H])([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(O)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Endothelin 1 (human, porcine)

溶解性	Soluble to 1 mg/ml in water

产品说明书 for Endothelin 1 (human, porcine)

分析证书/产品说明书

化学品安全技术说明书

参考文献 for Endothelin 1 (human, porcine)

参考文献是支持产品生物活性的出版物。

Inoue et al (1989) The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc.Natl.Acad.Sci.U.S.A. 86 2863 PMID: 2649896

Servitja et al (1998) Involvement of ET_A and ET_B receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes. Br.J.Pharmacol. 124 1728 PMID: 9756390

Yanagisawa et al (1988) Primary structure, synthesis, and biological activity of rat endothelin, and endothelium-derived vasoconstrictor peptide. Proc.Natl.Acad.Sci.U.S.A. 85 6964 PMID: 3045827

Yanagisawa and Masaski (1989) Molecular biology and biochemistry of the endothelins. TiPS 10 374 PMID: 2690429

Matsumoto et al (1996) Endothelin-induced changes of second messengers in cultured human ciliary muscle cells Invest.Ophthalmol.Vis.Sci. 37 1058 PMID: 8631621

Xiong et al (2001) Endothelin-1 stimulates leptin production in adipocytes. J.Biol.Chem. 276 28471 PMID: 11359784

Maguire and Davenport et al (1995) ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br.J.Pharmacol. 115 191 PMID: 7647976

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16 篇 Endothelin 1 (human, porcine) 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Endothelin 1 (human, porcine) 的部分引用包括：

Needham et al (2014) The role of K+ and Cl- channels in the regulation of retinal arteriolar tone and blood flow. J Pharmacol Exp Ther 55 2157 PMID: 24609622

Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762

Zheng et al (2017) Gastrodin Inhibits Store-Operated Ca(2+) Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol 8 222 PMID: 28487655

Giachini et al (2009) Interleukin-10 attenuates vascular responses to endothelin-1 via effects on ERK1/2-dependent pathway. Am J Physiol Heart Circ Physiol 296 H489 PMID: 19074677

Schafer et al (2017) IL-11 is a crucial determinant of cardiovascular fibrosis. Nature 552 110 PMID: 29160304

Suri et al (2010) Quercetin and its major metabolites selectively modulate cyclic GMP-dependent relaxations and associated tolerance in pig isolated coronary artery. Br J Pharmacol 159 566 PMID: 20050852

Ban et al (2019) S-nitrosation impairs KLF4 activity and instigates endothelial dysfunction in pulmonary arterial hypertension. Redox Biol 21 101099 PMID: 30660098

Yuan et al (2015) Endothelial cells enhance the migration of bovine meniscus cells. J Neurosci 67 182 PMID: 25307081

Yuan et al (2018) Dynamics and Functional Role of Dopaminergic Neurons in the Ventral Tegmental Area during Itch Processing. J Neurosci 38 9856 PMID: 30266741

Bellono et al (2014) UV light activates a Gαq/11-coupled phototransduction pathway in human melanocytes. J Gen Physiol 143 203 PMID: 24470488

Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol 171 5682 PMID: 25091502

Zhuang et al (2018) Fasudil preserves lung endothelial function and reduces pulmonary vascular remodeling in a rat model of end-stage pulmonary hypertension with left heart disease. Int J Mol Med 42 1341 PMID: 29901088

Hamby et al (2012) Inflammatory mediators alter the astrocyte transcriptome and calcium signaling elicited by multiple G-protein-coupled receptors. Invest Ophthalmol Vis Sci 32 14489 PMID: 23077035

Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol 147 607 PMID: 16432510

McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652

Cirino et al (2003) Involvement of β 3-adrenergic receptor activation via cyclic GMP- but not NO-dependent mechanisms in human corpus cavernosum function. Arthritis Rheumatol 100 5531 PMID: 12707413

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