Biological Activity
Subtype-selective GABAA receptor partial agonist. Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.
Licensing Information
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
Compound Libraries
L-838,417 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 399.4 |
| Formula | C19H19F2N7O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 286456-42-6 |
| PubChem ID | 9908880 |
| InChI Key | BQDUNOMMYOKHEP-UHFFFAOYSA-N |
| Smiles | FC(C=CC(F)=C3)=C3C1=NN=C2N1N=C(OCC4=NC=NN4C)C(C(C)(C)C)=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.97 | 50 | |
| ethanol | 7.99 | 20mM with sonication |
Preparing Stock Solutions
The following data is based on the product molecular weight 399.4. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.5 mL | 12.52 mL | 25.04 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.5 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
McCabe et al (2004) Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 46 171 PMID: 14680756
McMahon and France (2006) Differential behavioural effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. Br.J.Pharmacol. 147 260 PMID: 16331290
Knabl et al (2008) Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature 451 330 PMID: 18202657
Keywords: L-838,417, supplier, Subtype-selective, GABAA, partial, agonists, Receptors, L838417, merck, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
