您好，欢迎来到试剂信息网！ [登录] [免费注册]
试剂信息网
发布求购
位置：首页 > 产品库 > GW 627368
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：
 
GW 627368
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。
GW 627368图片
CAS NO:439288-66-1
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
GW 627368 (GW 627368X) 是一种新型、强效和选择性竞争性前列腺素 EP4 受体拮抗剂，具有额外的人 TP 受体亲和力，对人前列腺素 EP4 和 TP 受体的 pKi 值分别为 7.0 和 6.8。
Cas No.439288-66-1
化学名2-(4-(4,9-diethoxy-1-oxo-1H-benzo[f]isoindol-2(3H)-yl)phenyl)-N-(phenylsulfonyl)acetamide
Canonical SMILESO=C1N(C2=CC=C(CC(NS(=O)(C3=CC=CC=C3)=O)=O)C=C2)CC(C1=C4OCC)=C(C5=CC=CC=C45)OCC
分子式C30H28N2O6S
分子量544.62
溶解度DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml,DMSO: 10 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GW627368 (GW627368X) is a novel, potent and selective competitive antagonist of prostanoid EP4 receptor with additional human TP receptor affinity, with pKi values of 7.0 and 6.8 for human prostanoid EP4 and TP receptors respectively[1].

GW627368 (GW627368X) appears to bind to human prostanoid TP receptors but not the TP receptors of other species[1].GW627368 (GW627368X) (10 μM) produces 100% inhibition of U-46619 (EC100)-induced aggregation (approximate pA2 approximately 7.0) in human washed platelets[1].GW627368 (GW627368X) is devoid of agonist activity and actually produced a significant and concentration-related reduction in basal cAMP levels with pIC50 value of 6.3[1].GW627368 (GW627368X) induces inhibition of proliferation and invasion of human SUM149 IBC tumor cells beginning at 0.1 μM, with inhibition of proliferation and invasion of MDA-MB-231 non-IBC cells at higher concentrations[2].

GW627368 (GW627368X) (0-15 mg/kg; p.o.; every alternate day for 28 days) shows significant tumor regression characterized by tumor reduction and induction of apoptosis[3].

References:
[1]. Wilson RJ, et al. GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist. Br J Pharmacol. 2006 Jun;148(3):326-39.
[2]. Robertson FM, et al. Molecular and pharmacological blockade of the EP4 receptor selectively inhibits both proliferation and invasion of human inflammatory breast cancer cells. J Exp Ther Oncol. 2008;7(4):299-312.
[3]. Parida S, et al. Molecular inhibition of prostaglandin E2 with GW627368X: Therapeutic potential and preclinical safety assessment in mouse sarcoma model. Cancer Biol Ther. 2015;16(6):922-32.