OX Receptor

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

OX Receptor产品

所有产品(5) OX Receptor拮抗剂(5)

目录号	产品描述	文献引用	实验数据
S7585	SB-334867 SB-334867 是一种选择性 orexin-1 (OX1) receptor 拮抗剂。	J Neuroinflammation, 2020, 17(1):187 Med Sci Monit, 2019, 25:2886-2895
S1545	SB408124 SB408124是一种非肽类OX1 receptor拮抗剂，作用于全细胞和膜，K_i分别为57 nM和27 nM，比作用于OX2受体选择性高50倍。	Nat Chem Biol, 2017, 13(2):235-242
S6726^New	MK1064 MK1064是选择性orexin 2 receptor拮抗剂，IC50为18 nM。
S2160	Almorexant HCl Almorexant HCl (ACT-078573)是口服有效的双重orexin receptor 拮抗剂，其作用于受体 OX1 和 OX2 的 IC50 分别为 6.6 nM 和 3.4 nM。	Cell Rep, 2020, 31(11):107779 Am J Physiol Heart Circ Physiol, 2017, 312(4):H808-H817 J Pharmacol Exp Ther, 2016, 358(3):492-501	(C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. **P<0.0001; P<0.001; P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).
S6717	TCS-OX2-29 TCX-OX2-29是OX2R 拮抗剂，pKi=7.5。对hOX2R的选择性比hOX1R高250倍以上，IC50分别为40 nM和>10000 nM。

目录号	产品描述	文献引用	实验数据
S7585	SB-334867 SB-334867 是一种选择性 orexin-1 (OX1) receptor 拮抗剂。	J Neuroinflammation, 2020, 17(1):187 Med Sci Monit, 2019, 25:2886-2895
S1545	SB408124 SB408124是一种非肽类OX1 receptor拮抗剂，作用于全细胞和膜，K_i分别为57 nM和27 nM，比作用于OX2受体选择性高50倍。	Nat Chem Biol, 2017, 13(2):235-242
S6726^New	MK1064 MK1064是选择性orexin 2 receptor拮抗剂，IC50为18 nM。
S2160	Almorexant HCl Almorexant HCl (ACT-078573)是口服有效的双重orexin receptor 拮抗剂，其作用于受体 OX1 和 OX2 的 IC50 分别为 6.6 nM 和 3.4 nM。	Cell Rep, 2020, 31(11):107779 Am J Physiol Heart Circ Physiol, 2017, 312(4):H808-H817 J Pharmacol Exp Ther, 2016, 358(3):492-501	(C) No significant changes were observed compared with PBS control (n = 5) when sSNA is measured as % range. Grouped data for the % range from every treatment group are compared. AXT at 75 mg/kg (n = 4) produced no effect on baseline sympathetic activity. (D) AXT at 30 mg/kg (n = 5) and 75 mg/kg (n = 5) attenuated the effect of intermittent orexin-A (10 pmol×10; n = 5) on sSNA. Statistical significance was determined using one-way analysis of variance followed by Holm-Sidak correction to compare the effects with the control. Data are expressed as mean±S.E.M. **P<0.0001; P<0.001; P <0.05. #P<0.05 compared with intermittent orexin-A (10 pmol×10).
S6717	TCS-OX2-29 TCX-OX2-29是OX2R 拮抗剂，pKi=7.5。对hOX2R的选择性比hOX1R高250倍以上，IC50分别为40 nM和>10000 nM。