SB-408124 - Orexin Receptor (OX Receptor) Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESB-408124Cat. No.: HY-70068CAS No.: 288150-92-5分式: CHFNO分量: 356.37作靶点: Orexin Receptor (OX Receptor)作通路: GPCR/G Protein; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50

2、 mg/mL (140.30 mM; Need ultrasonic)H2O : 90% corn oilSolubility: 2.5 mg/mL (7.02 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 SB408124肽类OX1受体拮抗剂，在全细胞和细胞膜分析中Ki为57 nM和27 nM，对OX2受体的抑制性50倍。REFERENCES1. Morairty SR, et al. Dual hypocretin receptor antagonism

3、is more effective for sleep promotion than antagonism of either receptoralone.PLoS One. 2012;7(7):e39131. Epub 2012 Jul 2.2. Melis MR, et al. Neuroendocrine regulatory peptide-1 and neuroendocrine regulatory peptide-2 influence differentially feeding and penileerection in male rats: sites of action

4、in the brain.Regul Pept. 2012 Aug 20;177(1-3):46-52. Epub 2012 May 2.3. Assisi L, et al. Expression and role of receptor 1 for orexins in seminiferous tubules of rat testis.Cell Tissue Res. 2012 Jun;348(3):601-7.Epub 2012 Mar 28.4. Kis GK, et al. The osmotically and histamine-induced enhancement of

5、the plasma vasopressin level is diminished byintracerebroventricularly administered orexin in rats.Pflugers Arch. 2012 Apr;463(4):531-6. Epub 2012 Feb 16.5. Langmead et al (2004) Characterisation of the binding of 3H-SB-674042, a novel nonpeptide antagonist, to the human orexin-1receptor. Br.J.Pharmacol. 141 340.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 02