L-838,417

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Cat.No. 3250 - L-838,417 | C19H19F2N7O | CAS No. 286456-42-6
Description: GABAA 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)
Datasheet
Citations (3)
Reviews
Literature

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.

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.97 50
ethanol 7.99 20 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 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 mL 5.01 mL 10.02 mL
5 mM 0.5 mL 2.5 mL 5.01 mL
25 mM 0.1 mL 0.5 mL 1 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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

Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem.Pharmacol. 158 339 PMID: 30121248


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Keywords: L-838,417, L-838,417 supplier, Subtype-selective, GABAA, partial, agonists, Receptors, L838417, merck, 3250, Tocris Bioscience

3 Citations for L-838,417

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

Gee et al (2010) Limiting activity at beta1-subunit-containing GABAA receptor subtypes reduces ataxia. J Pharmacol Exp Ther 332 1040 PMID: 19940102

De la Luz-Cuellar et al (2019) Blockade of spinal α5-GABAA receptors differentially reduces reserpine-induced fibromyalgia-type pain in female rats. Eur J Pharmacol PMID: 31181208

Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248


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