L-838,417

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

Tocris Bioscience a Bio-Techne Brand

Catalog # 3250

Citations (3)

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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

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
Knabl Reversal of pathological pain through specific spinal GABA_A receptor subtypes. Nature 2008 PMID: 18202657
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
McCabe Subtype-selective GABAergic drugs facilitate extinction of mouse operant behaviour. Neuropharmacology 2004 PMID: 14680756

Citations for L-838,417 (3)

Showing 1 - 3 of 3 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for L-838,417 include:

De la Luz-Cuellar et al. (2019) Blockade of spinal α5-GABA_A receptors differentially reduces reserpine-induced fibromyalgia-type pain in female rats. Eur J Pharmacol. 858:172443
PMID: 31181208
Soderhielm et al. (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABA_A receptors. Biochem Pharmacol. 158:339
PMID: 30121248
Gee et al. (2010) Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther. 332:1040
PMID: 19940102

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