L-838,417
Tocris Bioscience, part of Bio-Techne | Catalog # 3250
GABAA partial agonist; displays subtype selectivity
Key Product Details
Description
GABAA partial agonist; displays subtype selectivity
Product Description
L-838,417 is a 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)Product Specifications
Molecular Weight
399.40
Formula
C19H19F2N7O
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
3-(2,5-Difluorophenyl)-7-(1,1-dimethylethyl)-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.97 | 50 |
Preparing Stock Solutions
for L-838,417
The following data is based on the product molecular weight 399.40
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 |
|---|---|---|---|
| 0.5 mM | 5.01 mL | 25.04 mL | 50.08 mL |
| 2.5 mM | 1.00 mL | 5.01 mL | 10.02 mL |
| 5 mM | 0.50 mL | 2.50 mL | 5.01 mL |
| 25 mM | 0.10 mL | 0.50 mL | 1.00 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Soderhielm Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 2018 PMID: 30121248
- McMahon and France Differential behavioural effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. Br.J.Pharmacol. 2006 PMID: 16331290
- Knabl Reversal of pathological pain through specific spinal GABAA receptor subtypes. Nature 2008 PMID: 18202657
- McCabe Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 2004 PMID: 14680756
Product Specific Notices for L-838,417
For research use only
Loading...
Loading...