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SB-334867 free base
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。
SB-334867 free base图片
CAS NO:792173-99-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
SB-334867 free base (SB334867A free base) 是一种优异的选择性和血脑屏障可透过性orexin-1 (OX1) 受体拮抗剂,比 OX2 (pKb=7.4) 具有选择性,是 5-HT2B 的 100 倍,5- HT2C 的 pKi 值分别为 5.4 和 5.3 。
Cas No.792173-99-0
别名1-(2-甲基苯并[D]噁唑-6-基)-3-(1,5-萘啶-4-基)脲,SB334867A free base
化学名1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea
Canonical SMILESCC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4
分子式C17H13N5O2
分子量319.32
溶解度≥ 14.55mg/mL in DMSO
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

SB-334867 free base is a selective antagonist of orexin-1 receptor [1].

Orexin-A and orexin-B are two peptides isolated from rat hypothalamus. They are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle.

SB-334867 free base could inhibit the orexin-A and orexin-B induced calcium responses in CHO-OX1 cells with pKB values of 7.27 and 7.23, respectively. SB-334867 was more selective for OX1 receptor over OX2 receptor. It caused 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. Moreover, SB-334867 was found to reduce both orexin-A-induced and fasting-induced food intake. The acute anorectic effect of it was associated with significant reductions in all active behaviours [1, 2].

References:
[1] Smart D, Sabido-David C, Brough S J, et al.  SB-334867-A: the first selective orexin-1 receptor antagonist. British journal of pharmacology, 2001, 132(6): 1179-1182.
[2] Rodgers R J, Halford J C G, Nunes de Souza R L, et al.  SB-334867, a selective orexin-1 receptor antagonist, enhances behavioural satiety and blocks the hyperphagic effect of orexin-A in rats. European Journal of Neuroscience, 2001, 13(7): 1444-1452.