EWP 815

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 In Vitro 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. 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. 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female mice (20 g)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%. Form:Solid IC50& Target:Ins(1,4)P2 phosphatase,Ins(1,4,5)P3 5-phosphatase, ,dopamine β-hydroxylase

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