Art. -Nr.: HY-108682

EMPA

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

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

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Reinheit: 99.92%
CAS. Nr.: 680590-49-2
Formel: C₂₃H₂₆N₄O₄S
Molecular Weight:454.54

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

EMPA Chemical Structure

CAS. Nr.: 680590-49-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target^[1]

OX₂ Receptor

Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen :

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 K_i values of 1.10±0.24 nM and 1.45±0.13 nM, respectively^[1].
EMPA shows an IC₅₀=5.75 µM, K_i=2.63 µM, and IC₅₀=12.8 µM, K_i=5.8 µM in the binding assay at human and mouse V_1a 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 680590-49-2
Appearance Solid
Molecular Weight 454.54
Formel C₂₃H₂₆N₄O₄S
Color White to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (14)

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Journal Impact Factor

Cardiovasc Res

Off-target effects of sodium-glucose co-transporter 2 blockers: empagliflozin does not inhibit Na+/H+ exchanger-1 or lower [Na+]i in the heart. [Abstract]

2021 Dec 17;117(14):2794-2806. PMID: 33135077
Metabolism

The early metabolic cardiac targets of empagliflozin during the development of heart failure, independent of SGLT2 inhibition. [Abstract]

2026 Feb 16:178:156568. PMID: 41707753
Cardiovasc Diabetol

SGLT2 inhibitor downregulates ANGPTL4 to mitigate pathological aging of cardiomyocytes induced by type 2 diabetes. [Abstract]

2024 Dec 4;23(1):430. PMID: 39633372
Biomed Pharmacother

Sodium glucose co-transporter 2 inhibitor empagliflozin prevents endothelial dysfunction induced by oscillatory shear stress. [Abstract]

2025 Oct 22:192:118670. PMID: 41130096
Antioxidants (Basel)

Empagliflozin Ameliorates Diabetic Cardiomyopathy by Inhibiting Ferroptosis via SIRT3: Mechanisms and Therapeutic Implications. [Abstract]

2026 Apr 24;15(5):543. PMID: 42193166
J Clin Transl Hepatol

1,5-Anhydroglucitol Aggravates Acute Liver Failure via the PPARα Signaling Pathway. [Abstract]

2026 Mar 28;14(3):291-300. PMID: 41970189
Biochim Biophys Acta Mol Basis Dis

SGLT2i delays c-Myc-induced HCC progression via targeting mTOR. [Abstract]

2025 Jun;1871(5):167805. PMID: 40113049
Am J Physiol Heart Circ Physiol

Empagliflozin treatment rescues abnormally reduced Na currents in ventricular cardiomyocytes from dystrophin-deficient mdx mice. [Abstract]

2024 Feb 1;326(2):H418-H425. PMID: 38099845
Biogerontology

Empagliflozin improves kidney senescence induced by D-galactose by reducing sirt1-mediated oxidative stress. [Abstract]

2023 Oct;24(5):771-782. PMID: 37227544
Sci Rep

SGLT2 inhibition with empagliflozin attenuates retinal oxidative stress and damage in diabetic mice. [Abstract]

2026 May 29. PMID: 42215540
Diabetol Metab Syndr

New insights into the role of empagliflozin on diabetic renal tubular lipid accumulation. [Abstract]

2022 Aug 23;14(1):121. PMID: 35999610
J Toxicol

Empagliflozin Alleviates Arsenic Trioxide-Induced Nephrotoxicity by Activating the SIRT1/Akt/Nrf2 Pathway. [Abstract]

2026 Feb 13:2026:5808911. PMID: 41695613
Research Square Preprint

2021 Sep.
Research Square Preprint

2021 Sep.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (110.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2000 mL

11.0001 mL

22.0003 mL

5 mM

0.4400 mL

2.2000 mL

4.4001 mL

10 mM

0.2200 mL

1.1000 mL

2.2000 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. P Malherbe, et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX₂ receptor. Br J Pharmacol. 2009 Apr; 156(8): 1326-1341.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2000 mL	11.0001 mL	22.0003 mL	55.0007 mL
	5 mM	0.4400 mL	2.2000 mL	4.4001 mL	11.0001 mL
	10 mM	0.2200 mL	1.1000 mL	2.2000 mL	5.5001 mL
	15 mM	0.1467 mL	0.7333 mL	1.4667 mL	3.6667 mL
	20 mM	0.1100 mL	0.5500 mL	1.1000 mL	2.7500 mL
	25 mM	0.0880 mL	0.4400 mL	0.8800 mL	2.2000 mL
	30 mM	0.0733 mL	0.3667 mL	0.7333 mL	1.8334 mL
	40 mM	0.0550 mL	0.2750 mL	0.5500 mL	1.3750 mL
	50 mM	0.0440 mL	0.2200 mL	0.4400 mL	1.1000 mL
	60 mM	0.0367 mL	0.1833 mL	0.3667 mL	0.9167 mL
	80 mM	0.0275 mL	0.1375 mL	0.2750 mL	0.6875 mL
	100 mM	0.0220 mL	0.1100 mL	0.2200 mL	0.5500 mL

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EMPA

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) EMPA

Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EMPA

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) EMPA

Alle Orexin Receptor (OX Receptor) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

EMPA Related Classifications

HY-108682 Related Classifications