Plecanatide (Synonyms:普卡那肽)
目录号 : KM4443 CAS No. : 467426-54-6 纯度 : 98%

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 (guanylate cyclase-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 190 nM。Plecanatide 在小鼠结肠炎模型中具有抗炎活性。

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生物活性

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.

IC50&Target

EC50: 190 nM (guanylate cyclase-C)

体外研究

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.

体内研究

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.
分子式
C65H104N18O26S4
分子量
1681.89
CAS号
467426-54-6
中文名称
普卡那肽
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
临床试验
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