Halopemide

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Halopemide  纯度: 99.65%

Halopemide 是一种有效的磷脂酶 D (PLD) 抑制剂,对人 PLD1 和 PLD2 的 IC50 分别为 220 和 310 nM。Halopemide 是多巴胺受体拮抗剂,是一种精神药物。

Halopemide

Halopemide Chemical Structure

CAS No. : 59831-65-1

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生物活性

Halopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent[1][2].

IC50 & Target[1][2]

PLD1

220 nM (IC50)

PLD2

310 nM (IC50)

dopamine receptors

 

体外研究
(In Vitro)

Halopemide (1-2 μM; 21 day) affects calcification in transdifferentiated MOVAS cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Halopemide (10 mg/kg; p.o.) induces dyskinesias in the majority of monkeys tested[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

416.88

Formula

C21H22ClFN4O2

CAS 号

59831-65-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [1]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17.

    [2]. Neale R, et al. Acute dyskinesias in monkeys elicited by halopemide, mezilamine and the “antidyskinetic” drugs, oxiperomide and tiapride. Psychopharmacology (Berl). 1981;75(3):254-7.

    [3]. Skafi N, et al. Phospholipase D: A new mediator during high phosphate-induced vascular calcification associated with chronic kidney disease. J Cell Physiol. 2019 Apr;234(4):4825-4839.

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