Plecanatide acetate(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽)

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Plecanatide acetate;(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽) 纯度: 99.26%

Plecanatide acetate 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 细胞中，EC50 值为 190 nM。Plecanatide acetate 可用于慢性特发性便秘的研究，在小鼠结肠炎模型中具有抗炎活性。

Plecanatide acetateamp;;(Synonyms: 普卡那肽醋酸盐；醋酸普卡那肽)

Plecanatide acetate Chemical Structure

CAS No. : 1075732-84-1

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5 mg ￥4900 In-stock
10 mg ￥8500 In-stock
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生物活性

Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis[1][2][3].

IC50 Target

EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)[1]
体外研究
(In Vitro)

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

MCE 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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c mice (2-4 month old) are induced colitis by TNBS[1]
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.

Clinical Trial

分子量

1741.94

Formula

C67H108N18O28S4
CAS 号

1075732-84-1
Sequence

Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu (Disulfide bridge: Cys4-Cys12; Cys7-Cys15)
Sequence Shortening

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

普卡那肽醋酸盐；醋酸普卡那肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
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.

    [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.