Home GPCR & G Protein OX Receptor antagonist EMPA For research use only.

EMPA

EMPA is a selective OX2 receptor antagonist and binds to human and rat OX2-HEK293 membranes with Kd values of 1.1 and 1.4 nM respectively.

EMPA Chemical Structure

EMPA Chemical Structure

CAS: 680590-49-2

Selleck's EMPA has been cited by 1 publication

Purity & Quality Control

Batch: E010701 DMSO] 91 mg/mL] false] Ethanol] 23 mg/mL] false] Water] Insoluble] false Purity: 99.79%
99.79

EMPA Related Products

Signaling Pathway

OX Receptor Signaling Pathways

OX Receptor Signaling Pathway

Choose Selective OX Receptor Inhibitors

Biological Activity

Description EMPA is a selective OX2 receptor antagonist and binds to human and rat OX2-HEK293 membranes with Kd values of 1.1 and 1.4 nM respectively.
Targets
human OX2 receptor [1] rat OX2 receptor [1]
1.1 nM(Kd) 1.4 nM(Kd)
In vitro
In vitro

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.[1]
Cell Research Cell lines HEK293-hOX2-cells
Concentrations 10 μM
Incubation Time 1 h
Method

The affinity of EMPA is assessed in membranes from HEK293-hOX2-cells using saturation and binding kinetics. The antagonist properties of EMPA are determined by Schild analysis using the orexin-A-or orexin-B-induced accumulation of inositol phosphates (IP).
In Vivo
In vivo
EMPA dose-dependently reverses [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice. EMPA 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]

Chemical Information & Solubility

Molecular Weight 454.54 Formula

C23H26N4O4S
CAS No. 680590-49-2 SDF --
Smiles CCN(CC1=CC=CN=C1)C(=O)CN(C2=CC=C(OC)N=C2)[S](=O)(=O)C3=CC=CC=C3C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 91 mg/mL ( (200.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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