EWP 815

Research use only, not for human use.

EWP 815 is a disulfiram analogue that functions as a powerful inhibitor of Ins(1,4) P 2 phosphatase, Ins(1,4,5) P 3 5-phosphatase, and dopamine β-hydroxylase activity .

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.

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.

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%.

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Metabolic Enzyme/Protease

Phosphatase

Phosphatase | Hydroxylase

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20231-01-0

350.59

C12H22N4S4

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (142.62 mM; Ultrasonic )

C(SSC(=S)N1CCN(C)CC1)(=S)N2CCN(C)CC2

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(-20℃)

With Ice Pack

≥ 2 years