Plecanatideacetate是一种鸟苷酸环化酶C受体(guanylatecyclase-C(GC-C)receptor)激动剂，能够结合并激活GC-C受体，在T84细胞中，EC50值为190nM。在小鼠结肠炎模型中，Plecanatideacetate具有抗炎活性。
CAS：1075732-84-1
分子式：C67H108N18O28S4
分子量：1741.94
纯度：98%
存储：Store at -20°C

Background:

Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, binds and activates GC-C receptor, with an EC50 of 190 nM in T84 cells. Plecanatide acetate shows an-inflammatory activity in models of murine colitis[1].

Plecanatide acetate is a guanylate cyclase-C (GC-C) receptor agonist, binds and activates GC-C receptor, with an EC50 of 190 nM in T84 cells[1].

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[1].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[1].|| Animal Model:|Female BALB/c mice (2-4 month old)[1]|Dosage:|0.5 and 2.5 mg/kg|Administration:|P.O. for 7 days, with the first dose given the same day as TNBS|Result:|Effectively reduced colitis severity scores in BALB/c mice.|| Animal Model:|BDF-1 mice (10-12 week old)[1]|Dosage:|0.005-5 mg/kg|Administration:|P.O. once daily for 7 days|Result:|Effective at 0.005 mg/kg as sulfasalazine (80 mg/kg) to ameliorate DSS induced colitis in BDF-1 mice, but had no incremental effect on the amelioration of colitis at higher doses than 0.005 mg/kg. Plecanatide at 0.05 mg/kg per day was as effective as 80 mg/kg per day of sulfasalazine.|| Animal Model:|TCRα-/- mice (sixteen week old)[1]|Dosage:|0.5 or 2.5 mg/kg|Administration:|P.O. for 14 days|Result:|Reduced colitis scores in TCRα-/- mice.

[1]. Shailubhai K, et al. Plecanatide and dolcanatide, novel guanylate cyclase-C agonists, ameliorate gastrointestinal inflammation in experimental models of murine colitis. World J Gastrointest Pharmacol Ther. 2015 Nov 6;6(4):213-22.