GW6471

製品コードS2798 バッチS279802

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₅H₃₆F₃N₃O₄
	分子量	619.67	CAS No.	880635-03-0
Solubility (25°C)*	体外	DMSO	100 mg/mL (161.37 mM)
		Ethanol	20 mg/mL (32.27 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	GW 6471は、IC50が0.24 μMのPPARαの強力なアンタゴニストです。
in vitro	GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. This compound at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. It adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes. This chemical at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα.
in vivo	GW6471 is a potent PPARα antagonist.

製品説明

GW 6471は、IC50が0.24 μMのPPARαの強力なアンタゴニストです。

in vitro

GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. This compound at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. It adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes.

This chemical at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα.

in vivo

GW6471 is a potent PPARα antagonist.

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assays
キナーゼアッセイ	The effects of GW6471 on the interaction of coactivator and co-repressor peptides with PPAR are determined by chemical-mediated fluorescence energy transfer assays. The experiments are conducted with 5 nM PPARα LBD of biotinylated peptide containing individual motifs , following the manufacturer
細胞アッセイ	細胞株	Cell-free assays
	濃度	0.24 μM
	反応時間
	実験の流れ
動物実験	動物モデル	Male athymic Nu/Nu mice
	投薬量	20 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/11845213/
https://pubmed.ncbi.nlm.nih.gov/17439719/
https://pubmed.ncbi.nlm.nih.gov/22190909/

https://pubmed.ncbi.nlm.nih.gov/18724387/
https://pubmed.ncbi.nlm.nih.gov/25810260/

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sorafenib enhanced the function of myeloid-derived suppressor cells in hepatocellular carcinoma by facilitating PPARα-mediated fatty acid oxidation [ Mol Cancer, 2025, 24(1):34]	PubMed: 39876004
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Nutrient deficiency-induced downregulation of SNX1 inhibits ferroptosis through PPARs-ACSL1/4 axis in colorectal cancer [ Apoptosis, 2025, 30(5-6):1391-1409]	PubMed: 40095264
Formononetin ameliorates depression-like behaviors through rebalancing microglia M1/M2 polarization and inhibiting NLRP3 inflammasome: involvement of activating PPARα-mediated autophagy [ Mol Med, 2025, 31(1):153]	PubMed: 40275171
Berberine Attenuates Nonalcoholic Hepatic Steatosis by Regulating Lipid Droplet-Associated Proteins: In Vivo, In Vitro and Molecular Evidence [ J Cell Mol Med, 2025, 29(7):e70524]	PubMed: 40194991
FNDC4 Prevents Aging-Related Cardiac Dysfunction: By Restoring AMPKα/PPARα-Dependent Mitochondrial Function [ JACC Basic Transl Sci, 2025, 10(7):101222]	PubMed: 40464727
Suppression of ferroptosis by vitamin A or radical-trapping antioxidants is essential for neuronal development [ Nat Commun, 2024, 15(1):7611]	PubMed: 39218970
CD24 negativity reprograms mitochondrial metabolism to PPARα and NF-κB-driven fatty acid β-oxidation in triple-negative breast cancer [ Cancer Lett, 2024, 587:216724]	PubMed: 38373689
Tubular CPT1A deletion minimally affects aging and chronic kidney injury [ JCI Insight, 2024, 9(6)e171961]	PubMed: 38516886
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419]	PubMed: 38097734

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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