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SB408124
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。
SB408124图片
CAS NO:288150-92-5
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SB408124 是一种非肽 OX1 受体拮抗剂，在全细胞和膜中的 Kis 值分别为 57 nM 和 27 nM。
Cas No.288150-92-5
化学名1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea
Canonical SMILESCC1=NC2=C(C=C(C=C2C(=C1)NC(=O)NC3=CC=C(C=C3)N(C)C)F)F
分子式C19H18F2N4O
分子量356.38
溶解度≥ 35.4 mg/mL in DMSO with gentle warming, ≥ 1.76 mg/mL in EtOH with ultrasonic and warming
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

SB408124 is a potent and novel nonpeptide antagonist of orexin-1 (OX(1)) receptor with Ki values of 27 nM and 57 nM in membrane formats and in whole cell, respectively. SB408124 was 50-fold selective over the human OX2 receptor [1].

Pre-treated with SB408124 before orexin A in primary astrocyte cultures from the rat cerebral cortex remarkably decreased the orexin A stimulatory activity on forskolin and basal-induced cAMP production [2].

In rats, SB408124 at dose of 30 μg/10 μl together with orexin-A after histamine (HA) or hypertonic saline injection could prevent the orexin-A-induced reduction in vasopressin (VP) concentration increase [3].

References:
[1] Langmead CJ1, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ.Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004 Jan;141(2):340-6.
[2] Woldan-Tambor A1, Biegańska K, Wiktorowska-Owczarek A, Zawilska JB. Activation of orexin/hypocretin type 1 receptors stimulates cAMP synthesis in primary cultures of rat astrocytes. Pharmacol Rep. 2011;63(3):717-23.
[3] Kis GK1, Molnár AH, Daruka L, Gardi J, Rákosi K, László F, László FA, Varga C.The osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. Pflugers Arch. 2012 Apr;463(4):531-6.

 
 
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