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MEN 10376
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。
MEN 10376图片
CAS NO:135306-85-3
包装:1mg
市场价:2436元

产品介绍
Men 10376 是一种选择性速激肽 NK-2 受体拮抗剂，对大鼠小肠 NK-2 受体的 Ki 值为 4.4 μM。
Cas No.135306-85-3
别名Neurokinin-2 receptor antagonist
化学名(3S,6S,9R,12R,15S,18S,21R)-9,15,18-tris((1H-indol-3-yl)methyl)-3,25-diamino-21-carbamoyl-6-(4-hydroxybenzyl)-12-isopropyl-4,7,10,13,16,19-hexaoxo-5,8,11,14,17,20-hexaazapentacosan-1-oic acid
Canonical SMILESO=C([C@@H](C(C)C)NC([C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](CC(C=C3)=CC=C3O)NC([C@H](CC(O)=O)N)=O)=O)=O)N[C@H](C(N[C@H](C(N[C@@H](C(N)=O)CCCCN)=O)CC4=CNC5=CC=CC=C45)=O)CC6=CNC7=CC=CC=C67
分子式C57H68N12O10
分子量1081.24
溶解度Water : 1.43 mg/mL (1.20 mM)
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

Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.

Men 10376 is a selective tachykinin NK-2 receptor, with a Ki of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (Ki, >10 μM)[1]. Men 10376 shows pA2s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (Ki, >10 μM)[2].

Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats[2].

References:
[1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.
[2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.