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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC 50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis
In Vitro
Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cGMP synthesis in a dose-dependent manner with EC 50 of 190 nM in T84 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Plecanatide (0.5 and 2.5 mg/kg, p.o.) ameliorates spontaneous and chemically induced colitis after treatment for 7 days in BALB/c mice, and 14 days in TCRα -/- mice . Plecanatide (0.005-5 mg/kg, once daily for 7 days) also shows anti-inflammatory activity in dextran sulfate sodium (DSS) and trinitrobenzene sulfonic (TNBS)-induced colitis in BDF-1 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice (2-4 month old) are induced colitis by TNBS Dosage: 0, 0.5 and 2.5 mg/kg Administration: P.o. for 7 days Result: Effectively reduced colitis severity scores as compared to vehicle treatment.
Form:Solid
IC50& Target:EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)