Plecanatide

Research use only, not for human use.

Plecanatide acetate is an analogue of Uroguanylin. It is an orally active guanylate cyclase-C (GC-C) receptor agonist.

Plecanatide acetate is an analogue of Uroguanylin. It is an orally active guanylate cyclase-C (GC-C) receptor agonist. (In Vitro):Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cyclic guanosine monophosphate (cGMP) synthesis in a dose-dependent manner with EC50 of 190 nM in T84 cells.(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.

Plecanatide (1 nM-10 μM) activates GC-C receptor to stimulate cyclic guanosine monophosphate (cGMP) synthesis in a dose-dependent manner with EC50 of 190 nM in T84 cells.

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. 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.

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Metabolic Enzyme/Protease

Guanylate Cyclase

guanylate cyclase-C

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467426-54-6

1681.89

C65H104N18O26S4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (59.46 mM)

CC(C)C[C@H](NC([C@H]1NC(CNC([C@@H](NC([C@H]2NC([C@H](C)NC([C@@H](NC([C@H](CC(N)=O)NC([C@@H](NC([C@H](CSSC1)NC([C@H](CC(C)C)NC([C@H](CCC(O)=O)NC([C@H](CSSC2)NC([C@H](CCC(O)=O)NC([C@H](CC(O)=O)NC([C@@H](N)CC(N)=O)=O)=O)=O)=O)=O)=O)=O)C(C)C)=O)=O)C(C)C)=O)=O)=O)[C@@H](C)O)=O)=O)=O)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years