JHU37152

製品コードS9789 バッチS978901

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₁₉H₂₀ClFN₄
	分子量	358.84	CAS No.	2369979-67-7
Solubility (25°C)*	体外	DMSO	72 mg/mL (200.64 mM)
		Ethanol	24 mg/mL (66.88 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	JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.
in vitro	JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.^[1]
in vivo	JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK-293 cells
	濃度	--
	反応時間	250 s
	実験の流れ	HEK-293 cells are transfected with 7 µg/dish of the cDNA encoding for hM3Dq or hM4Di and 7 µg/dish of GCaMP6. 48 hours after transfection, cells are harvested, washed, resuspended in Mg2+-free Locke's buffer pH 7.4 containing 5.6 mM of glucose and approximately 200,000 cells/well are distributed in black 96-well plates. Increasing concentrations of JHU37152 are added to the cells and fluorescence intensity (excitation at 480 nM, emission at 530 nM) is measured at 18-s intervals during 250 s using a PHERAstar FSX. The net change in intracellular Ca2+ concentration is expressed as F − F0 where F is the fluorescence at a given concentration of ligand and F0 is the average of the baseline values (fluorescence values of buffer-treated wells).
動物実験	動物モデル	6 week-old male wild-type C57BL/6J mice, 6 week-old male Sprague–Dawley rats
	投薬量	0.01 mg/kg - 0.3 mg/kg
	投与方法	IP

参考

[1] Jordi Bonaventura, et al. Nat Commun. 2019 Oct 11;10(1):4627.

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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