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SB-408124 Hydrochloride
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-408124 Hydrochloride图片
CAS NO:1431697-90-3
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
SB-408124 Hydrochloride 是一种选择性的非肽食欲素受体 1 (OX1) 受体拮抗剂，全细胞和膜的 Kis 值分别为 57 nM 和 27 nM。
Cas No.1431697-90-3
别名N-(6,8-二氟-2-甲基-4-喹啉基)-N'-[4-(二甲基氨基)苯基]脲盐酸盐,SB 408124 Hydrochloride;SB408124 Hydrochloride
化学名(Z)-N'-(6,8-difluoro-2-methylquinolin-4-yl)-N-(4-(dimethylamino)phenyl)carbamimidic acid hydrochloride
Canonical SMILESCC1=CC(/N=C(O)/NC2=CC=C(N(C)C)C=C2)=C3C=C(F)C=C(F)C3=N1.Cl
分子式C19H19ClF2N4O
分子量392.83
溶解度Soluble in DMSO
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

SB-408124 Hydrochloride is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.IC50 Value: 57 nM(Ki)Target: OX1 Receptorin vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.in vivo: SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).

References:
[1]. Langmead et al (2004) Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br.J.Pharmacol. 141 340.
[2]. Morairty SR, et al. Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone.PLoS One. 2012;7(7):e39131. Epub 2012 Jul 2.
[3]. Melis MR, et al. Neuroendocrine regulatory peptide-1 and neuroendocrine regulatory peptide-2 influence differentially feeding and penile erection in male rats: sites of action in the brain.Regul Pept. 2012 Aug 20;177(1-3):46-52. Epub 2012 May 2.
[4]. Assisi L, et al. Expression and role of receptor 1 for orexins in seminiferous tubules of rat testis.Cell Tissue Res. 2012 Jun;348(3):601-7. Epub 2012 Mar 28.
[5]. Kis GK, et al.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. Epub 2012 Feb 16.