EWP 815 是一种二硫类似物，是Ins(1,4)P2磷酸酶和Ins(1,4,5)P35-磷酸酶的有效抑制剂。EWP 815 也参与抑制体内多巴胺酶 β-羟化酶活性。

EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4) P 2 phosphatase and Ins(1,4,5) P 3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity [1] [2].

EWP 815 inhibits thyrotropin-releasing hormone (TRH; 0.03 mM)-stimulated inositol phospholipid breakdown without affecting basal breakdown rates in prelabelled GH 3 cells with IC 50 s of 83 mM (soluble enzymes) and 71 mM (particulate enzymes), respectively [1]. EWP 815 (30 μM; 1 h) exerts higher inhibition on Ins(1,4) P 2 phosphatase rather than Ins(1,4,5) P 3 5-phosphatase with the mean [ 3 H]Ins(1,4) P 2 /mean [ 3 H]Ins P recovery ratio of 2.6 [1]. EWP 815 (6, 8 μM; 10 min) inhibits dephosphorylation of [ 3 H]Ins(1,4,5) P 3 5-phosphatase in particulate and soluble fractions with IC 50 s of 6 μM and 8 μM, respectively [1]. EWP 815 (3-300 μM; 30 min) suppresses thyrotropin-releasing hormone (TRH)-stimulated (100 nM) inositol phospholipid production by 30% (100 μM) and 1.8% (300 μM), respectively, without affecting Ins(1,4,5) P 3 binding [1].

EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice [2]. Animal Model: Female mice (20 g) [2] Dosage: 50 mg/kg Administration: Intraperitoneal injection; 30 min before killed Result: Intraperitoneal injection; 30 min before killedInhibited β-hydroxylase of 3 H-α-methyldopamine. Reduced the amount of 3 H-α-Me-NA by 12%.

20231-01-0

C12H22N4S4

350.59

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years