VU 0357121

製品コードS2795 バッチS279501

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	C₁₇H₁₇F₂NO₂
	分子量	305.32	CAS No.	433967-28-3
Solubility (25°C)*	体外	DMSO	61 mg/mL (199.79 mM)
		Ethanol	21 mg/mL (68.78 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	VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.
in vitro	VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. ^[1] VU0357121 show weaker cooperativity in the Ca²⁺ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. ^[2]

製品説明

VU0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with EC50 of 33 nM, is inactive or very weakly antagonizing at other mGlu receptor subtypes.

in vitro

VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. ^[1] VU0357121 show weaker cooperativity in the Ca²⁺ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Radioligand Binding Assay
キナーゼアッセイ	The allosteric antagonist MPEP analogue [³H]methoxyPEPy is used to evaluate the ability of test compounds to interact with the MPEP site on mGlu5. Membranes are prepared from rat mGlu5 HEK293 cells. VU0357121 is diluted in assay buffer (50 mM Tris/0.9% NaCl, pH 7.4) to a 5× stock, and 100 μL of the test compound is added to each well of a 96 deep-well assay plate. Three hundred microliter aliquots of membranes diluted in assay buffer (20 μg/well) are added to each well. One hundred microliters of [³H]methoxyPEPy (2 nM final concentration) is added, and the reaction is incubated at room temperature for 1 h with shaking. After the incubation period, the membrane-bound ligand is separated from free ligand by filtration through glass-fiber 96-well filter plates. The contents of each well are transferred simultaneously to the filter plate and washed 3−4 times with assay buffer using a cell harvester. Forty microliters of scintillation fluid is added to each well and the membrane-bound radioactivity determine by scintillation counting. Nonspecific binding is estimated using 5 μM MPEP. Concentration−response curves are generated using a four parameter logistical equation in GraphPad Prism.

参考

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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