EMPA

Product NameEMPA
CAS680590-49-2
MFC23H26N4O4S
MW454.54
EINECS
MOL File680590-49-2.mol

Chemical Properties

Boiling point	660.7±65.0 °C(Predicted)
Density	1.280±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble to 100 mM in DMSO and to 100 mM in ethanol
form	Powder
pka	4.77±0.10(Predicted)
color	white to light brown
InChI	1S/C23H26N4O4S/c1-4-26(16-19-9-7-13-24-14-19)23(28)17-27(20-11-12-22(31-3)25-15-20)32(29,30)21-10-6-5-8-18(21)2/h5-15H,4,16-17H2,1-3H3
InChIKey	KJPHTXTWFHVJIG-UHFFFAOYSA-N
SMILES	[S](=O)(=O)(N(CC(=O)N(CC)Cc3cnccc3)c2cnc(cc2)OC)c1c(cccc1)C

Safety Information

Hazard Codes	Xn
Risk Statements	22
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Acute Tox. 4 Oral

Usage And Synthesis

Description

EMPA is an orexin 2 receptor (OX2R) antagonist (K_i = 1.1 nM). It is selective for OX2R over OX1R (K_i = 900 nM). EMPA inhibits orexin-A- and orexin-B-induced calcium mobilization (IC₅₀s = 8.8 and 7.9 nM, respectively) and increases orexin-A- and orexin-B-induced inositol phosphate accumulation (EC₅₀s = 1.1 and 2.4 nM, respectively) in CHO(dHFr^-) cells expressing recombinant human OX2R. It reduces spontaneous locomotor activity and orexin-B-induced hyperlocomotion in mice when administered at doses ranging between 10 and 300 mg/kg.

Uses

EMPA is a novel high-affinity, selective antagonist for the OX2 receptor.

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].

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.

IC 50

OX₂ Receptor

storage

Store at -20°C

References

[1] P MALHERBE. Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor[J]. British Journal of Pharmacology, 2009, 156 8: 1326-1341. DOI: 10.1111/j.1476-5381.2009.00127.x

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