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L-838417

SKU: orb1706003

Description

L-838417 is a subtype-selective benzodiazepine site ligand that acts as a partial agonist at GABAA receptors containing α2, α3, or α5 subunits and as an antagonist at α1-containing receptors. This pharmacological profile makes it a valuable research tool for investigating the roles of specific GABAA receptor subtypes in anxiety, sedation, and memory processes in both in vitro and in vivo studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number286456-42-6
MW399.4
Purity99.70%
FormulaC19H19F2N7O
SMILESFC=1C=CC(F)=C(C1)C2=NN=C3C=C(C(=NN32)OCC4=NC=NN4C)C(C)(C)C
TargetGABA Receptor
Solubility10% DMSO+90% Corn Oil:2 mg/mL (5.01 mM);DMSO:20 mg/mL (50.08 mM)

Bioactivity

Target IC50
α2β3γ2:0.67 nM (Ki)|α6β3γ2:2183 nM (Ki)|α3β3γ2:1.67 nM (Ki)|α5β3γ2:2.25 nM (Ki)|α1β3γ2:0.79 nM (Ki)|α4β3γ2:267 nM (Ki)
In Vivo
In unfamiliar environments, adult rats: at a dose of 1.0 mg/kg L-838417, social avoidance shifted to social preference and increased social probing. Adolescent rats: at 2.0 mg/kg L-838417 dose, elimination of social avoidance but no increase in social probing. In familiar environments (after repeated restraint stress), reversal of stress-induced anxiety effects, regardless of age, at 0.5 mg/kg L-838417 dose. ≥1.0 mg/kg L-838417 dose, reduced social probing, possibly related to inhibition of motor function.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

L 838417, L838417, L-838417, GABA, GABA Receptor, GABAReceptor

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Key Properties

No computed properties available.

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Protocol Information

L-838417 (orb1706003)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,170.00
5 mg
¥ 3,120.00
10 mg
¥ 3,510.00
25 mg
¥ 7,670.00
50 mg
¥ 11,310.00
100 mg
¥ 16,510.00
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