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Chemical Structure| 680590-49-2 Chemical Structure| 680590-49-2

Structure of EMPA
CAS No.: 680590-49-2

Chemical Structure| 680590-49-2

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EMPA is highly potent, selective OX2 receptor antagonist with IC50 values of 2.3 nM and 1900 nM for OX2 and OX1 respectively.

Synonyms: EMPA

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Product Details of EMPA

CAS No. :680590-49-2
Formula : C23H26N4O4S
M.W : 454.54
SMILES Code : N(C1=CN=C(C=C1)OC)(CC(=O)N(CC)CC1=CN=CC=C1)S(C1C=CC=CC=1C)(=O)=O
Synonyms :
EMPA
MDL No. :N/A

Safety of EMPA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human coronary artery endothelial cells (HCAECs) 1 μM 24 h EMPA ameliorates stretch induced oxidative stress and cell permeability via inhibiting PKC activity. Redox Biol. 2024 Feb;69:102979
BV2 microglia 50 μM 24 hours To evaluate the anti-inflammatory effects of EMPA on LPS-induced cell inflammation and NLRP3 inflammasome activation. Results showed that EMPA significantly suppressed the upregulation of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) mRNA levels and inhibited the expression of NLRP3 inflammasome-related proteins. J Neuroinflammation. 2023 Dec 12;20(1):296
Human coronary artery endothelial cells (HCAECs) 1 μM 24 hours EMPA reduces NOX activation and ROS generation induced by 10% stretch via inhibition of PKC activity Redox Biol. 2024 Feb;69:102979
H9C2 cardiomyocytes 0.04-5 μM 2 or 24 hours To evaluate the effect of EMPA on intracellular Na+ and Ca2+ concentrations, results showed that EMPA effectively suppressed the increase in intracellular Na+ and Ca2+ concentrations under high glucose conditions Exp Mol Med. 2023 Jun;55(6):1174-1181
HL-1 cells 10, 50, 500 nM 24 hours To evaluate the cytotoxic or cytoprotective effects of EMPA on cardiomyocytes. Co-incubation with EMPA increased cell viability, reduced intracellular Ca2+ content and oxidative stress. Cardiovasc Diabetol. 2021 Jul 23;20(1):150
H9C2 cells 1 µM 72 hours To investigate the effect of EMPA on IFN-γ-induced cell senescence, results showed that EMPA significantly inhibited IFN-γ-induced oxidative stress and senescence, and promoted cell proliferation. Cardiovasc Diabetol. 2024 Jul 23;23(1):269
Porcine coronary artery endothelial cells 100 nM 24 hours To evaluate the protective effect of EMPA on Ang II-induced endothelial senescence and dysfunction, results showed that EMPA inhibited Ang II-induced oxidative stress, increased senescence markers, and endothelial dysfunction. Cardiovasc Diabetol. 2021 Mar 16;20(1):65
human ventricular cardiac myoblasts AC16 0.5 µM 7 days To evaluate the effects of EMPA on high glucose-induced DNA methylation changes in the promoter regions of NF-κB and SOD2. Results showed that EMPA prevented HG-induced DNA demethylation by reducing TET2 binding to the promoter regions and restored normal gene expression levels. Cardiovasc Diabetol. 2023 Feb 2;22(1):24

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Diabetic and non-diabetic myocardial infarction models Oral 30 mg/kg/day 1 week or 24 hours pretreatment EMPA significantly reduced infarct size and myocardial fibrosis, improving cardiac function and survival rate. Protein Cell. 2022 May;13(5):336-359
C57BL/6J male mice Retinal ischemia and reperfusion (IR) injury model Intravitreal injection 100 µg/ml Single injection, observed for 7 days To evaluate the therapeutic efficacy of EMPA in retinal IR injury. Results showed that EMPA significantly protected retinal ganglion cells (RGCs) from IR injury, attenuated local retinal inflammation, and restored the expression of mitochondrial dynamics-related genes Mfn1 and Opa1. J Neuroinflammation. 2023 Dec 12;20(1):296
Rat Langendorff perfused heart model Perfusion 10 µM 10 min pretreatment followed by continuous perfusion To investigate the effects of EMPA on cardiac function and metabolism during ischemia/reperfusion. Results showed that EMPA improved left ventricular-developed pressure, increased ATP and phosphocreatine levels, and enhanced Gibbs free energy for ATP hydrolysis. Additionally, EMPA shifted cardiac metabolism from glucose oxidation to increased ketone utilization. Cardiovasc Res. 2023 Dec 19;119(16):2672-2680
Zebrafish DM-HFrEF model Immersion 0.2-5 μM From 5 dpf, lasting more than 24 hours To evaluate the effects of EMPA on survival, locomotion, and cardiac function in zebrafish, results showed that EMPA significantly improved survival, locomotion, and cardiac function Exp Mol Med. 2023 Jun;55(6):1174-1181
C57Bl/6 mice Non-diabetic mice Oral gavage 10 mg/kg/day Once daily for 10 days To evaluate the protective effects of EMPA against DOXO-induced cardiotoxicity. EMPA improved cardiac function, reduced cardiac fibrosis and expression of inflammatory markers. Cardiovasc Diabetol. 2021 Jul 23;20(1):150
C57BL/6J mice HFpEF model Oral gavage 10 mg/kg/day Once daily for 28 days To investigate the protective effect of EMPA on cardiac function in HFpEF mice, results showed that EMPA improved diastolic dysfunction, alleviated cardiac hypertrophy and fibrosis, and inhibited cardiac inflammation and aging processes. Cardiovasc Diabetol. 2024 Jul 23;23(1):269
Rats Aortic arch and thoracic aorta segments In vitro incubation 100 nM 15 hours To evaluate the inhibitory effect of EMPA on the upregulation of SGLT1 and SGLT2 protein expression in Ang II- and eNOS inhibitor-treated thoracic aorta segments, results showed that EMPA reduced oxidative stress and improved endothelial function. Cardiovasc Diabetol. 2021 Mar 16;20(1):65

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.00mL

2.20mL

1.10mL

22.00mL

4.40mL

2.20mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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