S85518 |
SB-674042 |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)