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EMPA

CAT: 0013-GTR19157737-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19157737-01Size:200 mg
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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) 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. 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.
CAS Number
680590-49-2
Purity
>98% (HPLC)
Solubility
DMSO:230 mg/mL (506 mM; Need ultrasonic)
Smiles
CCN (Cc1cccnc1) C (=O) CN (c1ccc (OC) nc1) S (=O) (=O) c1ccccc1C
Molecular Formula
C23H26N4O4S
Molecular Weight
454.54
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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