Syrosingopine

製品コードS9907 バッチS990702

化学情報

	Synonyms	Su-3118	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₃₅H₄₂N₂O₁₁
	分子量	666.71	CAS No.	84-36-6
Solubility (25°C)*	体外	DMSO	100 mg/mL (149.99 mM)
		Ethanol	16 mg/mL (23.99 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	Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
in vitro	Syrosingopine treatment leads to high intracellular lactate levels and thereby end-product inhibition of lactate dehydrogenase by inhibiting the Lactate Transporters MCT1 and MCT4. The loss of NAD+ regeneration capacity due to combined metformin and syrosingopine treatment results in glycolytic blockade, leading to ATP depletion and cell death. <sup><a class="sref" href="#s_ref">[1]</a></sup>
in vivo	Syrosingopine treatment leads to reduced serum lactate levels significantlyn, and higher intracellular lactate from liver tumor nodules in syrosingopine-treated liver tumor model mice. <sup><a class="sref" href="#s_ref">[1]</a></sup>

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCT116 cells, HeLa, HAP1
	濃度	10 μM
	反応時間	2 h
	実験の流れ	HCT116 cells are grown to 80% confluency in DMEM and pre-treated with compounds (10 μM) for 2 hours. After ishing with PBS, cytosolic depletion is performed by scraping cells and incubating with 1.9ml digitonin buffer for 30 minutes on ice.And then used for DARTS assay. For ATP and lactate measurement,HeLa and HAP1 are seeded at 15000 cells/well or 30000 cells/well. After Syrosingopine incubation, cells are ished with PBS and lysed with 22.5 μL HCl. Cell lysates are neutralized with 7.5 μL 1M Tris-base and incubated with 30 μL detection reagent. Luminescence is recorded after 1 hour and intracellular lactate concentrations determined from a standard curve.
動物実験	動物モデル	Liver-specific Tsc1 and Pten double-knockout mice
	投薬量	7.5 mg/kg
	投与方法	i.p.

参考

[1] Don Benjamin, et al. Cell Rep. 2018 Dec 11;25(11):3047-3058.e4.

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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