VUF 10166

製品コードS2865 バッチS286501

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	C₁₃H₁₅ClN₄
	分子量	262.74	CAS No.	155584-74-0
Solubility (25°C)*	体外	Ethanol	61 mg/mL (232.16 mM)
		DMSO	21 mg/mL (79.92 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	VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with K_i of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.
in vitro	VUF10166 shows low activity to 5-HT₃AB receptor with K_i of 22 nM. VUF10166 may be used to can distinguish between 5-HT₃A and 5-HT₃AB receptors. VUF10166 has no activity to α7 nACh receptor. VUF10166 also acts as a partial agonist at 5-HT3A receptors with EC50 of 5.2 μM, which shows that VUF10166 is unlikely to bind in the receptor pore. ^[1]

プロトコル(参考用のみ)

キナーゼアッセイ	Radioligand Binding
キナーゼアッセイ	Transfected HEK 293 cells are harvested into 1 mL of ice-cold HEPES buffer (10 mM, pH 7.4) and frozen. After thawing, they are washed with HEPES buffer and resuspended, and 50 μg of cell membranes is incubated in 0.5 mL of HEPES buffer containing [³H]granisetron for 5-HT₃ receptor studies and [³H]epibatidine for nACh receptor studies. Nonspecific binding is determined using 10 μM d-tubocurarine or 3 mM nicotine, respectively. For competition binding (eight point), reactions are incubated for at least 30 hours at 4 ℃. For 5-HT₃ receptor dissociation experiments, reactions are incubated with 1 nM [³H ]granisetron for 2 hours before the addition of 100 μM VUF10166. Reactions are terminated by vacuum filtration using a Brandel cell harvester onto GF/B filters presoaked in 0.3% polyethyleneimine. Radioactivity is determined by scintillation counting using a Beckman BCLS6500.

参考

[1] Thompson AJ, et al. J Pharmacol Exp Ther, 2012, 341(2), 350-9.

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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