2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. L-838417

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.

For research use only. We do not sell to patients.

L-838417 Chemical Structure

L-838417 Chemical Structure

CAS No. : 286456-42-6

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5 mg USD 409 In-stock
10 mg USD 655 In-stock
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Based on 1 publication(s) in Google Scholar

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L-838417 Related Antibodies

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Description

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[1].

IC50 & Target

Ki: 0.79 nM (α1β3γ2), 0.67 nM (α2β3γ2), 1.67 nM (α3β3γ2), 267 nM (α4β3γ2), 2.25 nM (α5β3γ2) and 2183 nM (α6β3γ2)[1].
In Vivo

L-838417 (1.0 mg/kg) produces anxiolytic effects in adult rat, as indexed by a transformation of social avoidance into preference and an increase in social investigation[2].
L-838417 (2.0 mg/kg) eliminates social avoidance, but has no anxiolytic effects on social investigation[2].
L-838417 (0.5 mg/kg) reverses the anxiogenic effects of prior stress regardless of age, but with doses ≥ 1 mg/kg decreases social investigation, an effect possibly due in part to locomotor-impairing effects of this compound[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female adolescent and adult Sprague–Dawley rats[2].
Dosage: 0, 0.5, 1.0, 2.0, or 4.0 mg/kg.
Administration: IP.
Result: Adolescents required a higher dose (2 mg/kg) to attenuate their social avoidance.
The lowest dose of 0.5 mg/kg was sufficient to reverse the anxiogenic effects of repeated restraint as reflected by a significant increase in the coefficient relative to vehicle-treated animals.
Molecular Weight

399.41

Formula

C19H19F2N7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (62.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5037 mL 12.5185 mL 25.0369 mL
5 mM 0.5007 mL 2.5037 mL 5.0074 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (5.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5037 mL 12.5185 mL 25.0369 mL 62.5923 mL
5 mM 0.5007 mL 2.5037 mL 5.0074 mL 12.5185 mL
10 mM 0.2504 mL 1.2518 mL 2.5037 mL 6.2592 mL
15 mM 0.1669 mL 0.8346 mL 1.6691 mL 4.1728 mL
20 mM 0.1252 mL 0.6259 mL 1.2518 mL 3.1296 mL
25 mM 0.1001 mL 0.5007 mL 1.0015 mL 2.5037 mL
30 mM 0.0835 mL 0.4173 mL 0.8346 mL 2.0864 mL
40 mM 0.0626 mL 0.3130 mL 0.6259 mL 1.5648 mL
50 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.2518 mL
60 mM 0.0417 mL 0.2086 mL 0.4173 mL 1.0432 mL
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L-838417 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-838417286456-42-6L838417L 838417GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorsocialavoidanceanxiogeniceffectsInhibitorinhibitorinhibit

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