Plecanatide|467426-54-6|(普卡那肽)-陌孚医药/Medlife

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Plecanatide (Synonyms: 普卡那肽)

目录号: PL01692 纯度: ≥98%

CAS No. :467426-54-6

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中文名称	Plecanatide
中文别名	普卡那肽;普卡那肽 Plecanatide
英文名称	Plecanatide
英文别名	L-asparaginyl-L-alpha-aspartyl-L-alpha-glutamyl-L-cysteinyl-L-alpha-Glutamyl-L-leucyl-L-cysteinyl-L-valyl-L-asparaginyl-L-valyl-L-alanyl-L-cysteinyl-L-threonylglycyl-L-cysteinyl-L-leucine cyclic (4→12),(7→15)-bis(disulfide);SP 304;Trulance;Plecanatide;7IK8Z952OK;Plecanatide [USAN:INN];Guanilib;GTPL9069;DB13170;[3-glutamic acid(D>E)]human uroguanylin;(3-Glutamic acid(D>E))human uroguanylin (UGN)
Cas No.	467426-54-6
分子式	C₆₅H₁₀₄N₁₈O₂₆S₄
分子量	1681.89
包装储存	Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

产品详情

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。

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 EC 50 of 190 nM in T84 cells assay. Plecanatide shows anti-inflammatory activity in models of murine colitis.

性状

Solid

IC50 & Target[1][2]

EC50: 190 nM (guanylate cyclase-C)

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

ClinicalTrial

SequenceShortening

NDECELCVNVACTGCL (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)

参考文献

[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.

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