GSK 1016790A

Cat. No. 6433 3 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 TRPV4 agonist; active in vivo

化学名： N-[(1S)-1-[[4-[(2S)-2-[[(2,4-Dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]benzo[b]thiophene-2-carboxamide

纯度： ≥97% (HPLC)

引用文献 (3)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GSK 1016790A

GSK 1016790A is a potent TRPV4 agonist; elicits Ca²⁺ influx in human and mouse TRPV4-expressing HEK cells (EC₅₀ values of 2.1 and 18 nM, respectively). Enhances insulin mRNA expression. Increases ERK1/2 phosphorylation and NO production. Exhibits no activity at TRPM8 and TRPA1 (20 μM) channels. Induces bladder overactivity in TRPV4^+/+ mice.

化合物库 for GSK 1016790A

GSK 1016790A is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for GSK 1016790A

分子量	655.61
公式	C₂₈H₃₂Cl₂N₄O₆S₂
储存	Store at -20°C
纯度	≥97% (HPLC)
CAS Number	942206-85-1
PubChem ID	23630211
InChI Key	IVYQPSHHYIAUFO-VXKWHMMOSA-N
Smiles	CC(C)C[C@H](NC(C1=CC2=CC=CC=C2S1)=O)C(N3CCN(CC3)C([C@H](CO)NS(=O)(C4=C(Cl)C=C(Cl)C=C4)=O)=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 GSK 1016790A

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	65.56	100
	ethanol	65.56	100

制备储备液 for GSK 1016790A

以下数据基于产品分子量 655.61。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.53 mL	7.63 mL	15.25 mL
5 mM	0.31 mL	1.53 mL	3.05 mL
10 mM	0.15 mL	0.76 mL	1.53 mL
50 mM	0.03 mL	0.15 mL	0.31 mL

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产品说明书 for GSK 1016790A

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GSK 1016790A

参考文献是支持产品生物活性的出版物。

Billert et al (2017) TRPV4 regulates insulin mRNA expression and INS-1E cell death via ERK1/2 and NO-dependent mechanisms. Cell Signal. 35 242 PMID: 28359774

Thorneloe et al (2008) N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinar J.Pharmacol.Exp.Ther. 326 432 PMID: 18499743

If you know of a relevant reference for GSK 1016790A, please let us know.

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关键词: GSK 1016790A, GSK 1016790A supplier, GSK1016790A, trpv4, transient, receptor, potential, channels, potent, selective, agonists, agonism, activators, vanilloid, TRPV, 6433, Tocris Bioscience

3 篇 GSK 1016790A 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GSK 1016790A 的部分引用包括：

Brant E et al (2021) Endothelial pannexin 1-TRPV4 channel signaling lowers pulmonary arterial pressure in mice. Elife 10 PMID: 34490843

Kwon et al (2023) TRPV4-Rho GTPase complex structures reveal mechanisms of gating and disease. Nat Commun 14 3732 PMID: 37353484

Stefanie et al (2020) The Effects of the Anti-aging Protein Klotho on Mucociliary Clearance. Front Med (Lausanne) 6 339 PMID: 32039219

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