名称 | EMPA |
描述 | EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively) |
体外活性 | EMPA displaces the EMPA binding from cell membranes containing human and rat OX2 receptors, with Ki values of 1.10±0.24 nM and 1.45±0.13 nM, respectively. EMPA shows an IC50=5.75 μM, Ki=2.63 μM, and IC50=12.8 μM, Ki=5.8 μM in the binding assay at human and mouse V1a receptors, respectively. In CHO(dHFr-) cells stably expressing hOX2 receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca2+]i response with IC50s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively. |
体内活性 | EMPA (3-30 mg/kg;i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats.EMPA (3-30 mg/kg;i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 230 mg/mL (506 mM), Sonication is recommended.
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关键字 | Hypocretin Receptor | Orexin Receptor (OX Receptor) | HCRT Receptor | EMPA | inhibit | Inhibitor |
相关产品 | L-368,899 hydrochloride | YNT-185 | IPSU | MK-3697 | Filorexant | DORA-22 | Orexin B, rat, mouse Acetate | OXA (17-33) acetate | PF3274167 | ACT-462206 | Seltorexant | TCS 1102 |
相关库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | GPCR靶点分子库 |