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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
200mg电议
500mg电议

产品介绍
SB-408124 Hydrochloride 是一种选择性的非肽类OX1受体拮抗剂,在全细胞和细胞膜分析中Ki为 57 nM 和 27 nM,比对 OX2 受体的抑制性高 50 倍。
生物活性

SB-408124 Hydrochloride is a selective non-peptideorexin receptor1 (OX1) receptorantagonist withKis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor[1].

IC50& Target

OX1Receptor

57 nM (Ki, in whole cell )

OX1Receptor

27 nM (Ki, in cell membrane)

体外研究
(In Vitro)

Primary neuronal cultures from the hypothalamus of newborn SD rats are incubated with orexin A (1 μM), orexin A (1 μM) together with SB-408124 (100 μM) for 6 h. Orexin A-induced increases in arginine vasopressin (AVP) mRNA levels (2.7-fold) are attenuated by SB-408124 (1.2-fold)[3].

体内研究
(In Vivo)

SB-408124 reduces anxiety after psychotraumatic exposure. Predator induces acute psychotraumatic exposure decrease corticoliberin level in the rat's amygdala. Intranasal administration of SB-408124 restores it closely to normal and has an anxiolytic effect on animal behaviour[2].
Bilateral paraventricular nucleus microinjection of SB-408124 (30 pmol/50 nL per side) results in a greater reduction in mean arterial pressure (MAP) in high-salt intake (-16 mmHg) compared with NS-fed (-4 mmHg) anesthetized Dahl salt-sensitive rats[3].

分子量

392.83

性状

Solid

Formula

C19H19ClF2N4O

CAS 号

1431697-90-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 1 mg/mL(2.55 mM;ultrasonic and warming and heat to 60℃)

DMSO :< 1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble or slightly soluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5456 mL12.7282 mL25.4563 mL
5 mM---------
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。