GSK1016790A

更新时间：2025-08-25 18:17:37

GSK1016790A结构式	常用名	GSK1016790A	英文名	GSK-1016790A
	CAS号	942206-85-1	分子量	655.61300
	密度	N/A	沸点	N/A
	分子式	C₂₈H₃₂Cl₂N₄O₆S₂	熔点	N/A
	MSDS	美版	闪点	N/A

GSK1016790A用途

GSK1016790A是有效的瞬时受体电位香草酸4 (TRPV4) 激活剂。

中文名	GSK1016790A
英文名	N-[(2S)-1-[4-[(2S)-2-[(2,4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide
英文别名	更多

描述	GSK1016790A是有效的瞬时受体电位香草酸4 (TRPV4) 激活剂。
相关类别	信号通路 >> 跨膜转运 >> TRP频道研究领域 >> 癌症
参考文献	[1]. Jin M et al. Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. PLoS One, 2011 Feb 14;6(2):e16713. [2]. MP Addison et al. NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. Pharmacol Rep, 2016 Jun, 68(3):620-6.

描述

GSK1016790A是有效的瞬时受体电位香草酸4 (TRPV4) 激活剂。

相关类别

信号通路 >> 跨膜转运 >> TRP频道

研究领域 >> 癌症

参考文献

[1]. Jin M et al. Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. PLoS One, 2011 Feb 14;6(2):e16713.

[2]. MP Addison et al. NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. Pharmacol Rep, 2016 Jun, 68(3):620-6.

分子式	C₂₈H₃₂Cl₂N₄O₆S₂
分子量	655.61300
精确质量	654.11400
PSA	176.23000
LogP	5.28510
InChIKey	IVYQPSHHYIAUFO-VXKWHMMOSA-N
SMILES	CC(C)CC(NC(=O)c1cc2ccccc2s1)C(=O)N1CCN(C(=O)C(CO)NS(=O)(=O)c2ccc(Cl)cc2Cl)CC1
外观性状	粉末
储存条件	-20℃

GSK1016790AMSDS英文版

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

Angiotensin II induces membrane trafficking of natively expressed transient receptor potential vanilloid type 4 channels in hypothalamic 4B cells.

Am. J. Physiol. Regul. Integr. Comp. Physiol. 307(8) , R945-55, (2014)

Transient receptor potential vanilloid family type 4 (TRPV4) channels are expressed in central neuroendocrine neurons and have been shown to be polymodal in other systems. We previously reported that ...

Opposing actions of TRPV4 channel activation in the lung vasculature.

Respir. Physiol. Neurobiol. 219 , 43-50, (2015)

Transient receptor potential vanilloid 4 (TRPV4) calcium channels are known to promote endothelium-dependent relaxation of mouse mesenteric arteries but TRPV4's role in the pulmonary vasculature is un...

A mutation in TRPV4 results in altered chondrocyte calcium signaling in severe metatropic dysplasia.

Am. J. Med. Genet. A 167A , 2286-93, (2015)

Transient receptor potential cation channel, subfamily V, member 4 (TRPV4) is a polymodal modulated non-selective cation channel required for normal development and maintenance of bone and cartilage. ...

实验名称：Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident pro...
来源：NCGC
靶标：N/A
External Id：SERCaMPGLuc-p1-antagonist

实验名称：Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resid...
来源：NCGC
靶标：N/A
External Id：SERCaMPGluc-f3-cellviability-42h

实验名称：Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum residen...
来源：NCGC
靶标：N/A
External Id：SERCaMPGLuc-f1_f3-antagonist

实验名称：Primary qHTS assay for inhibitors of alpha-synuclein gene (SNCA) expression
来源：NCGC
External Id：SNCA-p-activity-luciferase

实验名称：Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum reside...
来源：NCGC
靶标：N/A
External Id：SERCaMPGLuc-f3-counterscreen-19h

实验名称：Primary qHTS for Identification of Small Molecule Activators of Huntingtin-Antisense ...
来源：NCGC
External Id：huntington-HTTAS8-p1-FF-overN

实验名称：Cytotoxicity counterscreen for inhibitors of SARS-CoV-2 cell entry
来源：NCGC
靶标：N/A
External Id：TRND-SARS-CoV-2-cytotox-48hr

实验名称：Primary qHTS to identify inhibitors of SARS-CoV-2 cell entry
来源：NCGC
External Id：TRND-SARS-CoV-2-PP

实验名称：Quantitative High-Throughput drug screen in 47 multiple myeloma cell lines against th...
来源：NCGC
靶标：N/A
External Id：s-my-keats_OPM1-m4-1

实验名称：Solubility of the compound in saline
来源：ChEMBL
靶标：N/A
External Id：CHEMBL4400627

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