您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > BWX 46
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：
 
BWX 46
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。
BWX 46图片
CAS NO:172997-92-1
包装与价格：
包装价格(元)
1mg电议
5mg电议
25mg电议

产品介绍
NPY Y5 receptor agonist,potent and highly selective
Cas No.172997-92-1
化学名(S,S,S,1Z,1'Z,2S,2'S)-N'1,N''1'-((R,S,6S,6'S,7Z,7'Z,9S,9'S,10Z,10'Z,12S,12'S,13Z,13'Z,15S,15'S,16Z,16'Z,18R,18'R,19Z,19'Z,21S,21'S)-18,18'-(disulfanediylbis(methylene))bis(1-amino-12-(3-guanidinopropyl)-8,11,14,17,20-pentahydroxy-6-((Z)-hydroxy(((S)-1-hyd
Canonical SMILESCCC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CC=C(O)C=C1)([H])[C@@](CC)([H])C)([H])CC(O)=N)([H])CC(C)C)([H])CSSC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC2=CC=C(O)C
分子式C116H186N36O28S2
分子量2597.07
溶解度≥ 260.4 mg/mL in DMSO with ultrasonic,<12.99 mg/mL in Water,<12.99 mg/mL in EtOH
储存条件Desiccate 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

IC50: 0.5 nM for Y5

The actions of neuropeptide Y (NPY) are mediated by at least six G-protein coupled receptors denoted as Y1, Y2, Y3, Y4, Y5, and y6. Investigations using receptor selective ligands and receptor knock-out mice show that NPY effects on feeding are mediated by both Y1 and Y5 receptors. BWX 46 is a Y5 receptor selective agonist.

In vitro: BWX 46 selectively bound Y5 receptors, and inhibited cAMP synthesis by Y5 cells with potencies comparable to that of NPY. In addition, BWX 46 (10 μM) exhibited no significant effect on the cAMP synthesis by Y1, Y2, and Y4 cells. Thus, BWX 46 constitutes the lowest molecular weight Y5 selective agonist reported to date [1].

In vivo: Intrahypothalamic-injection of 30 and 40 μg of BWX 46 stimulated the food intake by rats in a gradual manner, reaching maximal level 8 h after injection. This response was similar to that exhibited by other Y5 selective agonists, but differed from that of NPY, which exhibited a rapider orexigenic stimulus within 1 h [1].

Clinical trial: Up to now, BWX 46 is still in the preclinical development stage.

Reference:
[1] Ambikaipakan Balasubramaniam, Sulaiman Sheriff, Weixu Zhai, William T.  Chance. Bis(31/31’){[Cys31, Nva34]NPY(27–36)-NH2}: a neuropeptide Y (NPY) Y5 receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides 23 (2002) 1485–1490