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SB-408124
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图片
CAS NO:288150-92-5
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素
产品介绍
SB408124 是一种 OX1 受体的非肽拮抗剂,在全细胞和膜中的 Ki 值分别为 57 和 27 nM,其选择性是 OX2 受体的 50 倍。

产品描述

SB408124 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.

体外活性

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. [1] 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. [2]

体内活性

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. [3] Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). [4]

Cas No.

288150-92-5

分子式

C19H18F2N4O

分子量

356.377

别名

N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素

储存和溶解度

DMSO:35.6 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years