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EMPA is a high-affinity, reversible and specific orexin OX2 receptor antagonist. It binds to OX2-HEK293 membranes in rats and humans with KD values of 1.1 and 1.4 nM respectively.
| Targets |
human OX2 receptor ( Kd = 1.1 nM ); rat OX2 receptor ( Kd = 1.4 nM )
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| ln Vitro |
EMPA competitively opposes the accumulation of [3H]inositol phosphates (IP) at hOX2 receptors that is induced by orexin A and orexin B with pA2 values of 8.6 and 8.8 respectively[1].
EMPA removes the [3H]EMPA binding from rat and human OX2 receptor-containing cell membranes, with Ki values of 1.45±0.13 nM and 1.10±0.24 nM, respectively[1]. EMPA binds to human and mouse V1a receptors with IC50 values of 5.75 µM, Ki=2.63 µM, and IC50 values of 12.8 µM, Ki=5.8 µM, respectively[1]. EMPA inhibits the [Ca2+]i response evoked by orexin-A or orexin-B in CHO(dHFr-) cells that are stably expressing hOX2 receptors, with IC50 values of 8.8±1.7 nM and 7.9±1.7 nM, respectively[1]. |
| ln Vivo |
EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala11,D-Leu15]orexin-B-induced hyperlocomotion without substantially altering locomotor activity (LMA) in male NMRI mice[1].
EMPA (3-30 mg/kg; i.p.) significantly and dose-dependently lowers the baseline LMA in both female and male Wistar rats. EMPA (3-30 mg/kg; i.p.) shows a definite dose-dependent suppression of spontaneous activity in contrast to animals given a vehicle treatment[1]. |
| Animal Protocol |
Male NMRI mice (20-30 g)
1, 3, 10, 30, 100, 300 mg/kg Injected i.p. at a volume of 10 mL/kg |
| References |
| Molecular Formula |
C₂₃H₂₆N₄O₄S
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|---|---|
| Molecular Weight |
454.54
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| Exact Mass |
454.17
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| Elemental Analysis |
C, 60.78; H, 5.77; N, 12.33; O, 14.08; S, 7.05
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| CAS # |
680590-49-2
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| Appearance |
Solid powder
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| SMILES |
CCN(CC1=CN=CC=C1)C(=O)CN(C2=CN=C(C=C2)OC)S(=O)(=O)C3=CC=CC=C3C
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| InChi Key |
KJPHTXTWFHVJIG-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
N-ethyl-2-[(6-methoxypyridin-3-yl)-(2-methylphenyl)sulfonylamino]-N-(pyridin-3-ylmethyl)acetamide
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| Synonyms |
EMPA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~91 mg/mL (110.0~200.2 mM)
Ethanol: ~23 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2000 mL | 11.0001 mL | 22.0003 mL | |
| 5 mM | 0.4400 mL | 2.2000 mL | 4.4001 mL | |
| 10 mM | 0.2200 mL | 1.1000 mL | 2.2000 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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