产品
编 号：F367546
分子式：C24H21FN4O2S
分子量：448.51
分子式：C24H21FN4O2S
分子量：448.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 483313-22-0
产品详情
生物活性：
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.
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.
体外研究：
SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells.SB-674042 (5 μM; 4 ℃ for 30 min, and 37 ℃ for 3 h) reduces the potency of CB1 receptor agonist (HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors.SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor.
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.
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.
体外研究：
SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells.SB-674042 (5 μM; 4 ℃ for 30 min, and 37 ℃ for 3 h) reduces the potency of CB1 receptor agonist (HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors.SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor.
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