| Name | EMPA |
| Description | 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) |
| In vitro | 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. |
| In vivo | 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 230 mg/mL (506 mM), Sonication is recommended.
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| Keywords | Hypocretin Receptor | Orexin Receptor (OX Receptor) | HCRT Receptor | EMPA | inhibit | Inhibitor |
| Inhibitors Related | 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 |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library |
United States
