货号	规格	价格	上海	北京	珠海	重庆	武汉
S83289-5mg	≥98%	￥450.00 S83289-5mg ￥450.00 3-5天	0 货期：3-5天	-	-	-	-
S83289-10mg	≥98%	￥740.00 S83289-10mg ￥740.00 3-5天	0 货期：3-5天	-	-	-	-
S83289-50mg	≥98%	￥2370.00 S83289-50mg ￥2370.00 3-5天	0 货期：3-5天	-	-	-	-
S83289-100mg	≥98%	￥3790.00 S83289-100mg ￥3790.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

SB-408124 Hydrochloride is a selective non-peptide orexin receptor 1 (OX1) receptor antagonist with Kis of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 Hydrochloride exhibits 50-fold selectivity over OX2 receptor

靶点：

OX1 Receptor:57 nM (Ki, in whole cell );OX1 Receptor:27 nM (Ki, in cell membrane);Others

体外研究：

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)

体内研究：

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. 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

参考文献：

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. I Tissen, et al. OX1R ANTAGONIST SB408124 ACTION AND EXTRAHYPOTHALAMIC CRF IN RATS AFTER PSYCHOTRAUMATIC EXPOSURE. Georgian Med News. 2019 May;(290):127-131. 3. Michael J Huber, et al. Increased activity of the orexin system in the paraventricular nucleus contributes to salt-sensitive hypertension. Am J Physiol Heart Circ Physiol. 2017 Dec 1;313(6):H1075-H1086.

溶解性：

Soluble in H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.546 ml	12.728 ml	25.456 ml
5 mM	0.509 ml	2.546 ml	5.091 ml
10 mM	0.255 ml	1.273 ml	2.546 ml
50 mM	0.051 ml	0.255 ml	0.509 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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浓度

体积

分子摩尔量

计算重置

SB-408124 (Hydrochloride)