EMPA
Tocris Bioscience, part of Bio-Techne | Catalog # 4558
Highly potent and selective OX2 antagonist; brain penetrant
Key Product Details
Description
Highly potent and selective OX2 antagonist; brain penetrant
Product Description
EMPA is a highly potent, selective OX2 receptor antagonist (IC50 values are 2.3 nM and 1900 nM for OX2 and OX1 respectively). Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX2-expressing CHO cells (IC50 values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant.Product Specifications
Molecular Weight
454.54
Formula
C23H26N4O4S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide
CAS Number
680590-49-2
PubChem ID
9981404
InChI Key
KJPHTXTWFHVJIG-UHFFFAOYSA-N
SMILES
O=C(CN(C2=CN=C(OC)C=C2)S(C3=C(C)C=CC=C3)(=O)=O)N(CC)CC1=CN=CC=C1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.45 | 100 | |
| Ethanol | 22.73 | 50 |
Preparing Stock Solutions
for EMPA
The following data is based on the product molecular weight 454.54
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.20 mL | 11.00 mL | 22.00 mL |
| 5 mM | 0.44 mL | 2.20 mL | 4.40 mL |
| 10 mM | 0.22 mL | 1.10 mL | 2.20 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Mochizuki Orexin receptor 2 expression in the posterior hypothalamus rescues sleepiness in narcoleptic mice. Proc.Natl.Acad.Sci.U.S.A 2011 PMID: 21368172
- Malherbe Mapping the binding pocket of dual antagonist almorexant to human orexin 1 and orexin 2 receptors: comparison with the selective OX1 antagonist SB-674042 and the selective OX2 antagonist N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene- Mol.Pharmacol. 2010 PMID: 20404073
- Malherbe Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX2 receptor. Br.J.Pharmacol. 2009 PMID: 19751316
Product Specific Notices for EMPA
For research use only
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