EMPA

Catalog No.E0107 Batch:E010701

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Technical Data

Formula

C23H26N4O4S

Molecular Weight 454.54 CAS No. 680590-49-2
Solubility (25°C)* In vitro DMSO 91 mg/mL (200.2 mM)
Ethanol 23 mg/mL (50.6 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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. 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]

Protocol (from reference)

Cell Assay:

[1]

  • 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).

Selleck's EMPA has been cited by 1 publication

Empagliflozin Ameliorates Diabetic Cardiomyopathy via Attenuating Oxidative Stress and Improving Mitochondrial Function [ Oxid Med Cell Longev, 2022, 2022:1122494] PubMed: 35585884

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.