GSK 2193874

Cat. No. 5106 9 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 and selective TRPV4 antagonist; orally active

化学名： 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide

纯度： ≥98% (HPLC)

引用文献 (9)

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 2193874

GSK 2193874 is a potent and selective TRPV4 antagonist (IC₅₀ values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca²⁺ influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarction in vivo models. Selective over a panel of ~200 human receptors, channels and enzymes. Orally active.

许可信息

Sold for research purposes under agreement from GlaxoSmithKline

化合物库 for GSK 2193874

GSK 2193874 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 2193874

分子量	691.62
公式	C₃₇H₃₈BrF₃N₄O
储存	Store at +4°C
纯度	≥98% (HPLC)
CAS Number	1336960-13-4
PubChem ID	53464483
InChI Key	UIVOZBSCHXCGPS-UHFFFAOYSA-N
Smiles	O=C(NC6(CC6)C5=CC=CC=C5)C2=C(CN4CCC(N7CCCCC7)CC4)C(C3=CC(C(F)(F)F)=CC=C3)=NC1=CC(Br)=CC=C12

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 2193874

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	34.58	50 温和加热

制备储备液 for GSK 2193874

以下数据基于产品分子量 691.62。 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
0.5 mM	2.89 mL	14.46 mL	28.92 mL
2.5 mM	0.58 mL	2.89 mL	5.78 mL
5 mM	0.29 mL	1.45 mL	2.89 mL
25 mM	0.06 mL	0.29 mL	0.58 mL

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产品说明书 for GSK 2193874

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 2193874

参考文献是支持产品生物活性的出版物。

Thorneloe et al (2012) An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci.Transl.Med. 4 159 PMID: 23136043

Cheung et al (2017) Discovery of GSK2193874: an orally active, potent, and selective blocker of transient receptor potential vanilloid 4. ACS Med.Chem.Lett. 8 549 PMID: 28523109

If you know of a relevant reference for GSK 2193874, please let us know.

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