L-838417
Based on 1 Customer Validation
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. L-838417 has anti-anxiety activity.
For research use only. We do not sell to patients.
- Purity: 98.73%
- CAS No.: 286456-42-6
- Formula: C19H19F2N7O
- Molecular Weight:399.41
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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].
L-838417 (2.0 mg/kg; i.p.)) eliminates social avoidance, but has no anxiolytic effects on social investigation[2].
L-838417 (0.5 mg/kg; i.p.)) 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.
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Animal Model:Male and female adolescent and adult Sprague-Dawley rats[2].
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Dosage:0, 0.5, 1.0, 2.0, or 4.0 mg/kg.
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Administration:IP.
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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.
Chemical Information
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CAS No. 286456-42-6
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Appearance Solid
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Molecular Weight 399.41
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Formula C19H19F2N7O
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Color White to off-white
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SMILES
CN1N=CN=C1COC2=NN3C(C=C2C(C)(C)C)=NN=C3C4=CC(F)=CC=C4F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Ciara McCabe, et al. Subtype-selective GABAergic drugs facilitate extinction of mouse operant behavior. Neuropharmacology. 2004 Feb;46(2):171-8. [Content Brief]
[2]. Melissa Morales, et al. Anxiolytic effects of the GABAA receptor partial agonist, L-838,417: Impact of age, test context familiarity, and stress. Pharmacol Biochem Behav. 2013 Aug;109:31-7. [Content Brief]
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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