Plecanatide acetate (Synonyms: 普卡那肽醋酸盐; 醋酸普卡那肽)
目录号: PL01693 纯度: ≥99%
CAS No. :1075732-84-1
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中文名称
Plecanatide acetate
英文名称
Plecanatide acetate
英文别名
Plecanatide acetate
Cas No.
1075732-84-1
分子式
C67H108N18O28S4
分子量
1741.94
包装储存
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
产品详情
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。
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 EC 50 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.
性状
Solid
IC50 & Target[1][2]
EC50: 190 nM (guanylate cyclase-C receptor, T84 cells)
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. 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)
Sequence
Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu (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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2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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