SB-674042

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB-674042 是非肽类食欲肽 OX1 受体拮抗剂 (Kd=5.03 nM)，对 OX1 受体的结合能力约是对 OX2 受体 100 倍，IC50 分别为 3.76 nM 和 531 nM。

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.

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.:Western Blot Analysis Cell Line:INS-1 cells Concentration:1 μM Incubation Time:24 hours; accompanied with 1 μM Orexin-A for 24 hour Result:Decreased the phosphorylation level of mTOR induced by Orexin-A.

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.

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Others

Other Targets

OX Receptor

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483313-22-0

448.51

C24H21FN4O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 25 mg/mL (55.74 mM; 超声助溶 )

Cc1nc(C(=O)N2CCC[C@H]2Cc2nnc(o2)-c2ccccc2)c(s1)-c1ccccc1F

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(-20℃)

With Ice Pack

≥ 2 years