EMPA

SKU: orb1219955

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)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. 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.

Key Properties

• CAS Number: 680590-49-2
• MW: 454.54
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₆N₄O₄S
• SMILES: CCN(Cc1cccnc1)C(=O)CN(c1ccc(OC)nc1)S(=O)(=O)c1ccccc1C
• Target: OX2 Receptor
• Solubility: DMSO:230 mg/mL (506 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  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. 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. Animal model: Male NMRI mice (20-30 g). Dosage: 1, 3, 10, 30, 100, 300 mg/kg. Administration: Injected i.p. at a volume of 10 mL/kg. Result: Dose-dependently reversed this [Ala11, D-Leu15]orexin-B-induced hyperlocomotionwithout itself significantly affecting LMA. Animal model: France and Male Wistar rats (196-237 g). Dosage: 3, 10, 30 mg/kg. Administration: Injected i.p. at a volume of 5 mL/kg. Result: Induced a significant and dose-dependent reduction in the baseline LMA. Demonstrated a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.
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• In Vitro:
  EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of[3H]inositol phosphates (IP) at hOX2 receptors with pA2 values of 8.6 and 8.8 respectively. EMPA displaces the [3H]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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

OX2 Receptor