Plecanatide acetate (C09-1164-523)

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 colitisIn VitroPlecanatide (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 VivoPlecanatide (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:SolidIC50& Target:EC50: 190 nM (guanylate cyclase-C receptor, T84 cells). Specifications and Purity: 99%. Molecular Formula: C67H108N18O28S4. Molecular Weight: 1741.94. PubChem CID: 168011839.