1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. EMPA

EMPA 

Cat. No.: HY-108682 Purity: >99.0%
Handling Instructions

EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively.

For research use only. We do not sell to patients.

EMPA Chemical Structure

EMPA Chemical Structure

CAS No. : 680590-49-2

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10 mM * 1 mL in DMSO USD 550 In-stock
Estimated Time of Arrival: December 31
1 mg USD 185 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively[1].

IC50 & Target[1]

OX2 Receptor

 

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[1].
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[1].
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[1].
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[1].

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[1].
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[1].

Animal Model: Male NMRI mice (20-30 g)[1]
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 hyperlocomotion without itself significantly affecting LMA.
Animal Model: France and Male Wistar rats (196-237 g)[1]
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.
Molecular Weight

454.54

Formula

C₂₃H₂₆N₄O₄S

CAS No.

680590-49-2

SMILES

O=C(N(CC)CC1=CC=CN=C1)CN(C2=CC=C(OC)N=C2)S(=O)(C3=CC=CC=C3C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

EMPAOrexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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