Home GPCR & G Protein OX Receptor antagonist EMPA

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EMPA OX Receptor antagonist

Cat.No.E0107

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 OX Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 454.54

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 454.54 Formula

C23H26N4O4S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 680590-49-2 -- Storage of Stock Solutions

Synonyms N/A Smiles CCN(CC1=CC=CN=C1)C(=O)CN(C2=CC=C(OC)N=C2)[S](=O)(=O)C3=CC=CC=C3C

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (200.2 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 23 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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

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Mechanism of Action

Targets/IC50/Ki
human OX2 receptor [1]
1.1 nM(Kd)
rat OX2 receptor [1]
1.4 nM(Kd)
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]
In vivo
EMPA dose-dependently reverses [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice. This compound induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats. It (3-30 mg/kg; i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.[1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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 --

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