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Urotensin II (114-124), human TFA Sale

目录号 : GC37871

Urotensin II (114-124), human TFA 是一种含有11个氨基酸的肽,能够通过结合孤儿G蛋白偶联受体14(GPR14)激活其必需的G蛋白偶联尿激肽II受体(UT),从而调节人类的心血管功能。

Urotensin II (114-124), human TFA Chemical Structure

Cas No.:251293-28-4

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Description

Urotensin II (114-124), human TFA is an 11-amino-acid peptide that stimulates its obligatory G protein-coupled urotensin II receptors (UT), by binding to the orphan G-protein-coupled receptor 14 (GPR14) to modulate cardiovascular function in humans[1-2].

In vitro, Urotensin II (114-124), human TFA at concentrations ranging from 10-13-10-7M has been used to treat arteries. Vasoconstrictive effects of Urotensin II (114-124), human TFA have been observed in isolated human coronary arteries (responders' data: −log[EC50] 10.05±0.46, Emax 15.39±6.53% of 100mM KCl contraction), mammary arteries (responders' data: −log[EC50] 9.71±0.90, Emax 16.41±6.15% of 100mM KCl contraction), and radial arteries (responders' data: −log[EC50] 9.52±0.83, Emax 19.65±6.26% of 100mM KCl contraction)[3]. Urotensin II (114-124), human TFA (1pM–0.1μM) has been shown to induce vasodilation in very small human pulmonary arteries[4]. Urotensin II (114-124), human TFA (10−7mol/L) stimulation of neonatal cardiac fibroblasts increased the level of mRNA transcripts for procollagens α1(I), α1(III), and fibronectin by 139±15% (P<0.01), 59±5% (P<0.05), and 141±14% (P<0.01), respectively, with a concomitant 23±2% increase in collagen peptide synthesis[5].

In vivo, Urotensin II (114-124), human TFA markedly increases total peripheral resistance in anaesthetized cynomolgus monkeys in a dose-dependent manner, a response associated with profound cardiac contractile dysfunction[6]. A biphasic cardiovascular response to bolus i.v. injection of human Urotensin II (114-124), human TFA (3nmol/kg) in conscious, male, Sprague-Dawley (SD) rats was identified, characterized by initial (0-5min) tachycardia, hypotension, and vasodilatation of the mesenteric and hindquarters arteries, followed by later (30-120min) tachycardia, hindquarters vasodilatation, and a modest rise in blood pressure[7].

References:
[1] Zhu YC, Zhu YZ, Moore PK. The role of urotensin II in cardiovascular and renal physiology and diseases. Br J Pharmacol. 2006;148(7):884-901.
[2] Russell FD. Urotensin II in cardiovascular regulation. Vasc Health Risk Manag. 2008;4(4):775-785.
[3] Maguire JJ, Kuc RE, Davenport AP. Orphan-receptor ligand human urotensin II: receptor localization in human tissues and comparison of vasoconstrictor responses with endothelin-1. Br J Pharmacol. 2000;131(3):441-446.
[4] Stirrat A, Gallagher M, Douglas SA, et al. Potent vasodilator responses to human urotensin-II in human pulmonary and abdominal resistance arteries. Am J Physiol Heart Circ Physiol. 2001;280(2):H925-H928.
[5] Tzanidis A, Hannan RD, Thomas WG, et al. Direct actions of urotensin II on the heart: implications for cardiac fibrosis and hypertrophy. Circ Res. 2003;93(3):246-253.
[6] Ames RS, Sarau HM, Chambers JK, et al. Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature. 1999;401(6750):282-286.
[7] Gardiner SM, March JE, Kemp PA, Bennett T. Bolus injection of human UII in conscious rats evokes a biphasic haemodynamic response. Br J Pharmacol. 2004;143(3):422-430.

Urotensin II (114-124), human TFA 是一种含有11个氨基酸的肽,能够通过结合孤儿G蛋白偶联受体14(GPR14)激活其必需的G蛋白偶联尿激肽II受体(UT),从而调节人类的心血管功能[1-2]

在体外,Urotensin II (114-124), human TFA 以10-13-10-7M的浓度范围用于处理动脉。在分离的人类冠状动脉(反应者数据:−log[EC₅₀] 10.05±0.46,最大效应为100mM KCl收缩的15.39±6.53%)、乳腺动脉(反应者数据:−log[EC₅₀] 9.71±0.90,最大效应为100mM KCl收缩的16.41±6.15%)和桡动脉(反应者数据:−log[EC₅₀] 9.52±0.83,最大效应为100mM KCl收缩的19.65±6.26%)中观察到Urotensin II (114-124), human TFA 的血管收缩效应[3]。在非常小的人类肺动脉中,Urotensin II (114-124), human TFA(1pM–0.1μM)被证明可以引起血管舒张[4]。Urotensin II (114-124), human TFA(10⁻⁷mol/L)刺激新生心肌成纤维细胞,使前胶原蛋白α1(I)、α1(III)和纤维连接蛋白的mRNA转录水平分别增加了139±15%(P<0.01)、59±5%(P<0.05)和141±14%(P<0.01),同时胶原蛋白肽合成增加了23±2%[5]

在体内,Urotensin II (114-124), human TFA(10–3000pmol/kg)以剂量依赖的方式显著增加了的食蟹猴的总外周阻力,这种反应与严重的心脏收缩功能障碍有关[6]。在清醒的雄性Sprague-Dawley(SD)大鼠中,通过静脉注射Urotensin II (114-124), human TFA(3nmol/kg)发现了双相心血管反应,其特征为初始阶段(0-5分钟)出现心动过速、低血压以及肠系膜和后肢动脉的血管扩张,随后在后期(30-120分钟)出现心动过速、后肢动脉扩张以及轻微的血压升高[7]

实验参考方法

In vitro experiment [1]:

Materials

human coronary arteries; mammary arteries; radial arteries

Preparation Method

Human arteries were cleaned of connective tissue and cut into 4mm rings. The luminal surface was gently rubbed with a metal probe to remove the endothelium. The vessels were then set up for isometric force recordings in 5ml organ baths containing oxygenated Kreb's solution at 37°C and allowed to equilibrate for 1 hour. Contractile responses to 100mM KCl were recorded at incrementally increasing levels of basal tension until no further increase in the KCl response was observed. This process determined the optimum resting tension for each preparation, which was followed by an additional 30 minutes equilibration period. Cumulative concentration–response curves were then constructed for Urotensin II (114-124), human TFA (10-13-10-7M). All experiments were terminated by the addition of 100mM KCl.

Reaction Conditions

10-13-10-7M

Applications

Urotensin II (114-124), human TFA contracted human coronary arteries (responders' data: −log[EC50] 10.05±0.46, Emax 15.39±6.53% of 100mM KCl contraction), mammary arteries (responders' data: −log[EC50] 9.71±0.90, Emax 16.41±6.15% of 100mM KCl contraction) and radial arteries (responders' data: −log[EC50] 9.52±0.83, Emax 19.65±6.26% of 100mM KCl contraction) with sub-nanomolar EC50 values.
Animal experiment [2]:

Animal models

cynomolgus monkeys (Macaca fascicularis)

Preparation Method

Adult male cynomolgus monkeys were treated with atropine sulphate (25µg/kg subcutaneous) and anaesthetized with ketamine (10mg/kg intramuscular). After endotracheal intubation, anaesthesia was maintained with 1–3% isoflurane. We prepared the animals for monitoring of systemic haemodynamics. Vehicle administration (0.9% NaCl) was followed by the cumulative administration of Urotensin II (114-124), human TFA. Isolated arterial rings from male cynomolgus monkeys (5kg) were suspended in organ baths containing Krebs (37°C; 95% O2; 5% CO2). Changes in isometric force were recorded under optimal resting tension. Cumulative agonist concentration–response curves were normalized to 60mM KCl or 1µM noradrenaline and fitted to a logistic equation. Unless stated otherwise, responses were measured in the presence of 10µM indomethacin using vessels denuded by rubbing (confirmed as a loss of dilator response to 10µM carbachol).

Dosage form

10–3000pmol/kg; i.v.; 0-10min

Applications

When administered intravenously at doses below 30pmol/kg, Urotensin II (114-124), human TFA, slightly increased cardiac output and reduced regional vascular resistance, with minimal changes in arterial blood pressure. In contrast, at doses ≥30pmol/kg, Urotensin II (114-124), human TFA decreased myocardial function and increased vascular resistance in a dose-dependent manner. Ultimately, doses within the range of 100–3000pmol/kg were lethal.

References:
[1] Maguire JJ, Kuc RE, Davenport AP. Orphan-receptor ligand human urotensin II: receptor localization in human tissues and comparison of vasoconstrictor responses with endothelin-1. Br J Pharmacol. 2000;131(3):441-446.
[2] Ames RS, Sarau HM, Chambers JK, et al. Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature. 1999;401(6750):282-286.

化学性质

Cas No. 251293-28-4 SDF
分子式 C66H86F3N13O20S2 分子量 1502.59
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 0.6655 mL 3.3276 mL 6.6552 mL
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