产品
编 号:F249518
分子式:C12H22N4S4
分子量:350.59
产品类型
结构图
CAS No: 20231-01-0
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产品详情
生物活性:
EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity.
体内研究:
EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice.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 3H-α-methyldopamine.Reduced the amount of 3H-α-Me-NA by 12%.
体外研究:
EWP 815 inhibits thyrotropin-releasing hormone (TRH; 0.03 mM)-stimulated inositol phospholipid breakdown without affecting basal breakdown rates in prelabelled GH3 cells with IC50s of 83 mM (soluble enzymes) and 71 mM (particulate enzymes), respectively.EWP 815 (30 μM; 1 h) exerts higher inhibition on Ins(1,4)P2 phosphatase rather than Ins(1,4,5)P3 5-phosphatase with the mean [3H]Ins(1,4)P2/mean [3H]InsP recovery ratio of 2.6. EWP 815 (6, 8 μM; 10 min) inhibits dephosphorylation of [3H]Ins(1,4,5)P3 5-phosphatase in particulate and soluble fractions with IC50s 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)P3 binding.