L-838,417

Name: L-838,417
Brand: Tocris Bioscience
SKU: 3250

Tocris Bioscience, part of Bio-Techne | Catalog # 3250

Citations (11)

COA / SDS

GABAA partial agonist; displays subtype selectivity

Key Product Details

Description:	GABA_A partial agonist; displays subtype selectivity
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
Purity:	≥98% (HPLC)
Molecular Weight:	399.4

View Full Technical Details for L-838,417

Technical Data
Citations

Biological Activity for L-838,417

L-838,417 is a subtype-selective GABA_A receptor partial agonist. Selectively binds to α1, α2, α3 and α5 subunits (K_i 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 for L-838,417

L-838,417 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for L-838,417

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for L-838,417

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	19.97	50

Preparing Stock Solutions for L-838,417

The following data is based on the product molecular weight 399.4.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will 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

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References for L-838,417

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 GABA_A receptors. Biochem.Pharmacol. 2018 PMID: 30121248
McMahon and France Differential behavioural effects of low efficacy positive GABA_A 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 GABA_A receptor subtypes. Nature 2008 PMID: 18202657
McCabe Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 2004 PMID: 14680756