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EMPA

Catalog No. T11186 CAS 680590-49-2

EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively)

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EMPA, CAS 680590-49-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 47.00
5 mg	In stock	$ 113.00
10 mg	In stock	$ 177.00
25 mg	In stock	$ 348.00
50 mg	In stock	$ 513.00
100 mg	In stock	$ 733.00
1 mL * 10 mM (in DMSO)	In stock	$ 133.00

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Purity: 99.91%

Biological Description

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Storage & Solubility Information

Description	EMPA is a selective, high-affinity and reversible antagonist of orexin OX2 receptor(human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively)
In vitro	EMPA displaces the EMPA binding from cell membranes containing human and rat OX2 receptors, with Ki values of 1.10±0.24 nM and 1.45±0.13 nM, respectively. EMPA shows an IC50=5.75 μM, Ki=2.63 μM, and IC50=12.8 μM, Ki=5.8 μM in the binding assay at human and mouse V1a receptors, respectively. 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.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 (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.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.

Molecular Weight	454.54
Formula	C23H26N4O4S
CAS No.	680590-49-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 230 mg/mL (506 mM), Sonication is recommended.

References and Literature

1. P Malherbe, et al. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library

Related Products

Related compounds with same targets

SB-674042 OXA (17-33) acetate PF3274167 YNT-185 IPSU Daridorexant hydrochloride Orexin B, rat, mouse Acetate Almorexant hydrochloride

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Keywords

EMPA 680590-49-2 GPCR/G Protein Neuroscience OX Receptor Hypocretin Receptor Orexin Receptor (OX Receptor) HCRT Receptor inhibit Inhibitor inhibitor

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