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Submit ReviewL-838,417
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)
Biological Activity for L-838,417
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)
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 Data for L-838,417
| 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 399.4. 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 for L-838,417
References for L-838,417
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
If you know of a relevant reference for L-838,417, please let us know.
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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 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 GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248
Do you know of a great paper that uses L-838,417 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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GABA Receptors Scientific Review
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.