货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S85518-5mg	≥99%	￥750.00 S85518-5mg ￥750.00 3-5天	0 货期：3-5天	-	-	-	-
S85518-10mg	≥99%	￥1260.00 S85518-10mg ￥1260.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S85518-5mg

≥99%

￥750.00

货期：3-5天

S85518-10mg

≥99%

￥1260.00

货期：3-5天

产品描述：

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively

靶点：

OX1 Receptor:3.76 nM (IC50);OX2 Receptor:531 nM (IC50);OX1 Receptor:1.1 nM (Ki);OX2 Receptor:129 nM (Ki)

体内研究：

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice Animal Model: Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g) Dosage: 0.3 nM/0.3 μL Administration: Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4) Result: Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.

参考文献：

1. Langmead CJ, et al. 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. Ellis J, et al. Orexin-1 receptor-cannabinoid CB1 receptor heterodimerization results in both ligand-dependent and -independent coordinated alterations of receptor localization and function. J Biol Chem. 2006 Dec 15;281(50):38812-24. 3. Chang X, et al. Orexin-A Stimulates Insulin Secretion Through the Activation of the OX1 Receptor and Mammalian Target of Rapamycin in Rat Insulinoma Cells. Pancreas. 2019 Apr;48(4):568-573. 4. Yaeger JDW, et al. Orexin 1 Receptor Antagonism in the Basolateral Amygdala Shifts the Balance From Pro- to Antistress Signaling and Behavior. Biol Psychiatry. 2022 May 1;91(9):841-852.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.23 ml	11.148 ml	22.296 ml
5 mM	0.446 ml	2.23 ml	4.459 ml
10 mM	0.223 ml	1.115 ml	2.23 ml
50 mM	0.045 ml	0.223 ml	0.446 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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