Orexin 2 Receptor Agonist

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Chemical Structure| 1796565-52-0 同义名 : OX2R
CAS号 : 1796565-52-0
货号 : A265471
分子式 : C32H34N4O5S
纯度 : 99%+
分子量 : 586.701
MDL号 : MFCD29924727
存储条件:

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 30 mg/mL(51.13 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Orexins A and B are a pair of neuropeptides that act on two G protein-coupled receptors, orexin receptor-1 (OX1R) and -2 (OX2R), to regulate sleep and wakefulness. Orexin 2 receptor agonist potently activates OX2R with an EC50 value of 23 nM compared to OX1R (EC50 of 1.616 μM). The Emax of orexin 2 receptor agonist against OX2R was 98%. In CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R, orexin 2 receptor agonist bound to hOX2R and hOX1R with Ki values of 0.14 μM and 0.77 μM, respectively[2]. In orexin receptor-expressing CHO cells, treatment of orexin 2 receptor agonist led to a robust Ca2+ response with 17.6-fold higher potency for OX2R than for OX1R. The response to orexin 2 receptor agonist was fully inhibited by 1 μM of Gq/11 inhibitor UBO-QIC. Orexin 2 receptor agonist also stimulated adenylyl cyclase activity in CHO cells treated with pertussis toxin and GF1092203X[3].
作用机制 The binding of orexin 2 receptor agonist to OX2R induces the inward movements of transmembrane helix 5 and 6, allowing the activity of orexin 2 receptor agonist against OX2R[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.52mL

1.70mL

0.85mL

17.04mL

3.41mL

1.70mL

参考文献

[1]Nagahara T, Saitoh T, et al. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015 Oct 22;58(20):7931-7.

[2]Nagahara T, Saitoh T, Kutsumura N, Irukayama-Tomobe Y, Ogawa Y, Kuroda D, Gouda H, Kumagai H, Fujii H, Yanagisawa M, Nagase H. Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists. J Med Chem. 2015 Oct 22;58(20):7931-7.

[3]Rinne MK, Leino TO, Turku A, Turunen PM, Steynen Y, Xhaard H, Wallén EAA, Kukkonen JP. Pharmacological characterization of the orexin/hypocretin receptor agonist Nag 26. Eur J Pharmacol. 2018 Oct 15;837:137-144.