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 No. 680590-49-2

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

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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05726032 Recruiting
Cirrhosis|Liver Failure
Yale University|Boehringer Ingelheim
 September 11 2023 Phase 2
NCT05553938 Recruiting
Heart Failure
Yale University
 August 4 2023 Phase 1
NCT05669742 Not yet recruiting
Sodium-glucose Transport Protein Two Inhibitor (SGLT2)Metabolic Deficits Caused by Antipsychotics
Tanta University
 January 2023 Phase 3
NCT04986735 Unknown status
Glycogen Storage Disease Type IB
Hong Kong Children''s Hospital
 August 8 2021 --

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy EMPA | EMPA supplier | purchase EMPA | EMPA cost | EMPA manufacturer | order EMPA | EMPA distributor