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TCS OX2 29
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。
TCS OX2 29图片
CAS NO:372523-75-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
TCS OX2 29 是一种有效的、高亲和力的选择性orexin-2 受体 (OX2R) 拮抗剂，IC50 值为 40 nM，pKI 值为 7.5。
Cas No.372523-75-6
化学名(S)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3,3-dimethyl-2-((pyridin-4-ylmethyl)amino)butan-1-one hydrochloride
Canonical SMILESO=C([C@H](C(C)(C)C)NCC1=CC=NC=C1)N(CC2=C3)CCC2=CC(OC)=C3OC.Cl
分子式C23H31N3O3
分子量397.51
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml
储存条件Store at -20℃
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

TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[1][2].

TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor[2].

TCS-OX2-29 (5-10 mg/kg; intraperitoneal injection; adult male NMRI mice) treatment suppresses conditioned place preference (CPP) acquisition and expression in both naive and dependent mice significantly[3].

References:
[1]. Hirose M et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidicantagonist. Bioorg Med Chem Lett, 2003 Dec 15, 13(24):4497-9.
[2]. Tabaeizadeh M, et al. The differential effects of OX1R and OX2R selective antagonists on morphine conditioned place preference in naive versus morphine-dependent mice. Behav Brain Res. 2013 Jan 15;237:41-8.
[3]. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363.