EMPA

SKU: orb1309708

Description

EMPA is a potent, selective, and reversible OX2 orexin receptor antagonist, exhibiting high affinity with KD values of 1.1 nM (human) and 1.4 nM (rat) in membrane binding assays. This compound is a valuable research tool for investigating sleep-wake regulation, narcolepsy, and metabolic disorders in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 680590-49-2
• MW: 454.54
• Purity: 99.91% (May vary between batches)
• Formula: C₂₃H₂₆N₄O₄S
• SMILES: N(S(=O)(=O)C1=C(C)C=CC=C1)(CC(N(CC=2C=CC=NC2)CC)=O)C=3C=CC(OC)=NC3
• Target: OX Receptor
• Solubility: DMSO:230 mg/mL (506.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (11 mM)

Bioactivity

• 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.
  Read more...
• 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.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EMPA, Hypocretin Receptor, HCRT Receptor, Inhibitor, inhibit, OX2, OX2 Receptor, OX Receptor, Orexin Receptor (OX Receptor), OXReceptor

Compound Identifiers

PubChem CID

9981404