Plecanatide (C09-1612-802)

Plecanatide, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide activates GC-C receptors to stimulate cGMP synthesis with an EC 50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitisIn VitroPlecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cyclic guanosine monophosphate (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). Specification: 0.98 Molecular Formula: C65H104N18O26S4 Molecular Weight: 1681.9 PubChem CID: 70693500 Isomeric SMILES: C[C@H]1C(=O)N[C@H]2CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC2=O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)C(C)C)CC(=O)N)C(C)C)CC(C)C)CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)N)N