SR-18292

製品コードS8528 バッチS852801

印刷

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

C₂₃ H₃₀ N₂O₂

分子量

366.50

CAS No.

2095432-55-4

Solubility (25°C)*

体外

DMSO

73 mg/mL (199.18 mM)

Ethanol

73 mg/mL (199.18 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

	5% DMSO 1 95% Corn oil	0.312mg/ml
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml

* <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	SR-18292 inhibits PGC-1α gluconeogenic activity and reduces co-activation of HNF4α by modulating the interaction between GCN5 and PGC-1α.
in vitro	SR-18292 is a potent inhibitor of the gluconeogenic gene expression and glucose production in hepatocytes. It increases the interaction of PGC-1α with GCN5 and reduces co-activation of HNF4α by PGC-1α. SR-18292 suppresses HNF4α/PGC-1α gluconeogenic transcriptional function^[2].
in vivo	SR-18292 reduces blood glucose, strongly increases hepatic insulin sensitivity and improves glucose homeostasis in dietary and genetic mouse models of type 2 diabetes. SR-18292 suppresses hepatic glucose production and increases liver insulin sensitivity in vivo. The liver is a major target of SR-18292 and probably accounts for a significant part of its anti-diabetic effects^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	U-2 OS cells overexpressing Ad-GCN5
	濃度	10 μM
	反応時間	18 h
	実験の流れ	For determination of GCN5 HAT activity U-2 OS cells overexpressing Ad-GCN5 are treated with SR-18292 (10μM) for 18 h. Cells are lysed with buffer B (20 mM HEPES-KOH (pH 7.9), 125 mM NaCl, 1 mM EDTA, 1 mM DTT, 1% IGEPAL (v/v), 10% glycerol (v/v), 5 mM NaF, 5 mM β-glycerophosphate, 5 mM sodium butyrate and 10 mM nicotinamide), supplemented with Protease Inhibitor Cocktail. FLAG-GCN5 is immunoprecipitated with FLAG beads overnight at 4℃ following multiple washes with lysis buffer. GCN5 is then eluted using 3× FLAG peptide and the purified protein is used to determine HAT activity using the HAT Inhibitor Screening Assay Kit.
動物実験	動物モデル	a high fat diet (HFD) fed mice, a dietary model of obesity and type 2 diabates
	投薬量	45 mg/kg
	投与方法	i.p.

参考

[1] Sharabi K, et al. Cell. 2017, 169(1):148-160.

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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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