您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Plecanatide acetate
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Plecanatide acetate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1075732-84-1
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
普卡那肽醋酸盐;醋酸普卡那肽
产品介绍
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 activeguanylate cyclase-C (GC-C) receptoragonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with anEC50of 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 EC50of 190 nM in T84 cells[1].

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].

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

性状

Solid

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-80°C2 years
-20°C1 year

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