GW 6471

Cat. No. 4618 38 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： PPARα antagonist

化学名： N-((2S)-2-(((1Z)-1-Methyl-3-oxo-3-(4-(trifluoromethyl)phenyl)prop-1-enyl)amino)-3-(4-(2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy)phenyl)propyl)propanamide

纯度： ≥98% (HPLC)

引用文献 (38)

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 GW 6471

GW 6471 is a PPARα antagonist (IC₅₀ = 0.24 μM). GW 6471 enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR. GW 6471 blocks SARS-CoV-2 infection in airway organoids (EC₅₀ = 2.1 μM) by blocking and downregulating the hypoxia inducible factor 1 subunit alpha (HIF1α) and HIF1 pathway; also reduces viral RNA. GW 6471 induces apoptosis and cell cycle arrest in kidney cancer cells.

许可信息

Sold with the permission of GlaxoSmithKline.

化合物库 for GW 6471

GW 6471 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 GW 6471

分子量	619.67
公式	C₃₅H₃₆F₃N₃O₄
储存	Store at +4°C
纯度	≥98% (HPLC)
CAS Number	880635-03-0
PubChem ID	446738
InChI Key	TYEFSRMOUXWTDN-DYQICHDWSA-N
Smiles	CC2=C(N=C(C4=CC=CC=C4)O2)CCOC(C=C1)=CC=C1C[C@@H](CNC(CC)=O)N/C(C)=C\C(C3=CC=C(C(F)(F)F)C=C3)=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 GW 6471

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	46.48	75
	ethanol	6.2	10

制备储备液 for GW 6471

以下数据基于产品分子量 619.67。 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
0.75 mM	2.15 mL	10.76 mL	21.52 mL
3.75 mM	0.43 mL	2.15 mL	4.3 mL
7.5 mM	0.22 mL	1.08 mL	2.15 mL
37.5 mM	0.04 mL	0.22 mL	0.43 mL

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产品说明书 for GW 6471

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GW 6471

参考文献是支持产品生物活性的出版物。

Xu et al (2002) Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα. Nature 415 813 PMID: 11845213

Muller et al (2009) An innovative method to study target protein-drug interactions by mass spectrometry. J.Med.Chem. 52 2875 PMID: 19379014

Duan et al (2021) An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection. Cell Rep. 37 PMID: 34731648

Aboud et al (2013) Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysis inhibition in kidney cancer cells. PLoS One 8 PMID: 23951092

If you know of a relevant reference for GW 6471, please let us know.

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关键词: GW 6471, GW 6471 supplier, GW6471, PPAR, PPARa, PPARalpha, PPARα, peroxisome, proliferator-activated, receptor, alpha, antagonists, GlaxoSmithKline, gsk, Receptors, Coronavirus, COVID-19, 4618, Tocris Bioscience