Plecanatide是尿鸟苷蛋白的类似物，是一种具有口服活性的鸟苷酸环化酶C受体(guanylatecyclase-C(GC-C)receptor)激动剂，在T84细胞实验中激活GC-C受体以刺激cGMP合成的EC50值为190nM。Plecanatide在小鼠结肠炎模型中具有抗炎活性。
货号:ajcx31314
CAS:467426-54-6
分子式:C65H104N18O26S4
分子量：1681.89
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 EC50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis[1][2][3].

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[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) are induced colitis by TNBS[1]

[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. [2]. Rao SSC. Plecanatide: a new guanylate cyclase agonist for the treatment of chronic idiopathic constipation. Therap Adv Gastroenterol. 2018 Jun 8;11:1756284818777945. [3]. Shailubhai K, et, al. Plecanatide, an oral guanylate cyclase C agonist acting locally in the gastrointestinal tract, is safe. Dig Dis Sci. 2013 Sep;58(9):2580-6.