L838417 | CAS#286456-42-6

MedKoo Cat#: 532101 | Name: L838417

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

L838417 is a GABAA receptor modulator.

Chemical Structure

L838417

CAS#286456-42-6

Theoretical Analysis

MedKoo Cat#: 532101

Name: L838417

CAS#: 286456-42-6

Chemical Formula: C19H19F2N7O

Exact Mass: 399.1619

Molecular Weight: 399.41

Elemental Analysis: C, 57.14; H, 4.80; F, 9.51; N, 24.55; O, 4.01

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Related CAS #

No Data

Synonym

L838417; L 838417; L-838417.

IUPAC/Chemical Name

5-({[7-tert-butyl-3-(2,5-difluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]oxy}methyl)-1-methyl-1H-1,2,4-triazole

InChi Key

BQDUNOMMYOKHEP-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H19F2N7O/c1-19(2,3)13-8-15-24-25-17(12-7-11(20)5-6-14(12)21)28(15)26-18(13)29-9-16-22-10-23-27(16)4/h5-8,10H,9H2,1-4H3

SMILES Code

CN1N=CN=C1COC2=NN3C(C=C2C(C)(C)C)=NN=C3C4=CC(F)=CC=C4F

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.

In vitro activity:

TBD

In vivo activity:

In Experiment 1, L-838,417 produced anxiolytic effects in rat adults at 1.0 mg/kg, as indexed by a transformation of social avoidance into preference and an increase in social investigation. Reference: Pharmacol Biochem Behav. 2013 Aug;109:31-7. https://pubmed.ncbi.nlm.nih.gov/23664899/

	Solvent	mg/mL	mM
Solubility
	DMSO	20.0	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 399.41 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
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Morales M, Varlinskaya EI, Spear LP. Anxiolytic effects of the GABA(A) receptor partial agonist, L-838,417: impact of age, test context familiarity, and stress. Pharmacol Biochem Behav. 2013 Aug;109:31-7. doi: 10.1016/j.pbb.2013.05.004. Epub 2013 May 8. PMID: 23664899; PMCID: PMC3765038. 2. McMahon LR, France CP. Differential behavioral effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys. Br J Pharmacol. 2006 Feb;147(3):260-8. doi: 10.1038/sj.bjp.0706550. PMID: 16331290; PMCID: PMC1751295.

In vitro protocol:

TBD

In vivo protocol:

1: Munro G, Ahring PK, Mirza NR. Developing analgesics by enhancing spinal inhibition after injury: GABAA receptor subtypes as novel targets. Trends Pharmacol Sci. 2009 Sep;30(9):453-9. doi: 10.1016/j.tips.2009.06.004. Review. PubMed PMID: 19729210.