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人内皮素3

人内皮素3用途

Endothelin-3, human, mouse, rabbit, rat 是由21个氨基酸组成的血管活性肽,可与G蛋白连接的跨膜受体,ET-RA 和ET-RB 结合。

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人内皮素3名称

[ CAS 号 ]:
117399-93-6

[ 中文名 ]:
人内皮素3

[ 英文名 ]:
Endothelin-3 (human, mouse, rabbit, rat) acetate salt

[中文别名 ]:

内皮素3

[英文别名 ]:

ET-3
MFCD00076378
Endothelin 3 human,rat
Endothelin-3, human
Endothelin-3, human, mouse, rabbit, rat

人内皮素3生物活性

[ 描述 ]:

Endothelin-3, human, mouse, rabbit, rat 是由21个氨基酸组成的血管活性肽,可与G蛋白连接的跨膜受体,ET-RA 和ET-RB 结合。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

多肽产品

研究领域 >> 心血管疾病

研究领域 >> 神经疾病

[ 靶点 ]

ET-RA, ET-RB[1]

[体外研究]

内皮素(ET)是包含三种不同同种型的21-氨基酸血管收缩肽家族：ET-1,ET2和内皮素-3。在血浆,心脏,脑和血管平滑肌细胞(VSMC)中检测到内皮素-3。 VSMCs的表面酶将大内皮素-3分解为相应的成熟肽内皮素-3。内皮素-3下调冠状动脉VSMC中的内皮素ETA受体表达,而不影响受体密度或功能性ETA受体反应。相反,高浓度的内皮素-3(100 nM)可增加ETB受体的表达,但可消除受体的血管收缩反应,这可能是由于内皮素-3的脱敏作用[1]。内皮素-3刺激ENCC与各种ECM组分的粘附。内皮素-3诱导ENCC形状和突出动力学的快速变化,有利于片状伪足的持续生长和稳定,这一过程与局灶粘连和活化的β1-整联蛋白的数量增加同时发生[2]。

[体内研究]

低浓度的内皮素-3可通过ETB2活化和NO产生减弱炎症反应。内皮素-3主要作用于ETB,在低浓度下特异性地抑制血小板活化因子(PAF)诱导的爪水肿,而ET-1和内皮素-2均作用于ETA和ETB,均表现出抑制活性。在BQ-123(分别为66.4±6.7％和65.4±22.6％)存在下,ET-1和内皮素-3(各0.5 pmol /爪)的抑制作用与内皮素-3(0.5 pmol/d)相当。单独使用(65.4±10.9％),而在BQ-788存在下ET-1和内皮素-3均未显示出抑制活性[3]。

[参考文献]

[1]. Skovsted GF, et al. Endothelin-1 and Endothelin-3 Regulate Endothelin Receptor Expression in Rat Coronary Arteries. Basic Clin Pharmacol Toxicol. 2015 Nov;117(5):297-305.

[2]. Gazquez E, et al. Endothelin-3 stimulates cell adhesion and cooperates with β1-integrins during enteric nervous system ontogenesis. Sci Rep. 2016 Dec 1;6:37877. doi: 10.1038/srep37877.

[3]. Sato A, et al. Endothelin-3 at low concentrations attenuates inflammatory responses via the endothelin B2 receptor. Inflamm Res. 2013 Apr;62(4):417-24.

[相关活性小分子]

人内皮素3物理化学性质

[ 分子式 ]:
C₁₂₁H₁₆₈N₂₆O₃₃S₄

[ 分子量 ]:
2643.04000

[ 精确质量 ]:
2641.11000

[ PSA ]:
1056.08000

[ LogP ]:
6.33930

[ 外观性状 ]:
powder | white

[ 储存条件 ]:
−20°C

人内皮素3安全信息

[ 安全声明 (欧洲) ]:
S22

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

人内皮素3文献

Involvement of endothelins in deoxycorticosterone acetate-salt hypertension through the modulation of noradrenergic transmission in the rat posterior hypothalamus.

Exp. Physiol. 100 , 617-27, (2015)

What is the central question of this study? Does ex vivo administration of endothelin-1 and endothelin-3 regulate noradrenergic transmission in the posterior hypothalamus of deoxycorticosterone acetat...

Direct conversion of mouse and human fibroblasts to functional melanocytes by defined factors.

Nat. Commun. 5 , 5807, (2014)

Direct reprogramming provides a fundamentally new approach for the generation of patient-specific cells. Here, by screening a pool of candidate transcription factors, we identify that a combination of...

Analysis of immunostaining and western blotting of endothelin 1 and its receptors in mitral stenosis.

Rev. Bras. Cir. Cardiovasc. 30 , 211-8, (2015)

Rheumatic Fever represents a serious public health problem in developing countries, with thousands of new cases each year. It is an autoimmune disease, which occurs in response to infection by strepto...

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