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

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

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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.

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

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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

Mechanism of Action

Targets/IC50/Ki
human OX2 receptor
1.1 nM(Kd)
rat OX2 receptor
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.
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.
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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