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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
L-822179 targets the α5 subunit-containing GABAA receptors, acting as a selective inverse agonist. GABAA receptors are ligand-gated chloride channels that mediate fast inhibitory neurotransmission in the brain. The α5 subunit is predominantly expressed in the hippocampus, a brain region critical for learning and memory. As an inverse agonist, L-822179 binds to the benzodiazepine site of the GABAA receptor and reduces the receptor's activity, thereby decreasing inhibitory neurotransmission. This mechanism is thought to enhance cognitive function.
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| ln Vitro |
In primary hippocampus cultures, α5IA (100 nM, 5 days) dramatically inhibits Aβ 1-42-induced cell death [1].
In vitro, L-822179 acts as a selective inverse agonist for the α5 subtype of the GABAA receptor, with a higher intrinsic activity at the α5 subtype than other drugs. Its selectivity for the α5 subunit over other GABAA receptor subtypes is a key feature of its profile. Detailed in vitro potency data, such as EC50 values for receptor modulation, are not extensively reported in the available literature. |
| ln Vivo |
Long-term recognition of spatial memory deficits and the ability of Ts65Dn to learn spatially can be sustainably restored by α5IA (5 mg/kg, ip, once) [2].
In vivo, L-822179 has been shown to enhance cognition in laboratory animals. It acts as an "alcohol antagonist," markedly reducing the amnesic effect of alcohol and partially attenuating sedation, similar to Ro15-4513, but without the anxiogenic effect. These in vivo activities confirm its potential as a cognitive enhancer and its utility in studying memory and alcohol-related disorders. |
| Enzyme Assay |
Non-cell-based receptor binding assays for L-822179 typically involve radioligand binding studies using membrane preparations from cells expressing the α5 subunit-containing GABAA receptors. The receptor is incubated with a radiolabeled benzodiazepine ligand and varying concentrations of L-822179. Binding affinity (Ki) is determined by measuring displacement of the radiolabeled ligand. Selectivity profiling against other GABAA receptor subtypes is performed to confirm specificity.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Primary mouse hippocampalculture Tested Concentrations: 0.3 nM, 3 nM, 30 nM, 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: At a concentration of 100 nM, Aβ 1-42-induced cell death was Dramatically diminished13 %. Dramatically reduces the expression of GABAAR α5 subunit. Cellular assays for L-822179 are performed using cells expressing α5 subunit-containing GABAA receptors. Cells are treated with the compound at various concentrations, and receptor activity is measured using electrophysiological techniques (patch-clamp) or fluorescence-based membrane potential assays. The compound's ability to modulate GABA-induced currents is quantified. These assays confirm its functional activity as an inverse agonist. |
| Animal Protocol |
In vivo animal models for L-822179 include studies of cognitive function in rodents, such as the Morris water maze or novel object recognition tests. The compound is administered via appropriate routes, and cognitive performance is assessed. Its effects on alcohol-induced amnesia and sedation are also studied in animal models. These studies confirm the compound's cognitive-enhancing and alcohol-antagonizing effects.
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| ADME/Pharmacokinetics |
L-822179 has a molecular weight of 362.35 g/mol and a molecular formula of C₁₇H₁₄N₈O₂. Its CAS number is 215874-86-5. The compound is supplied as a solid with a purity of >98% (HPLC). It is soluble in DMSO. Storage conditions: -20°C. The compound is supplied for research use only.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for L-822179 are not extensively reported in the available literature. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
L-822179 is also known as α5IA and alpha5IA. It is a selective inverse agonist for the α5 subtype of the GABAA receptor. It enhances cognition in laboratory animals without being proconvulsant or anxiogenic. It acts as an "alcohol antagonist," reducing the amnesic effect of alcohol. It is a research tool for studying cognitive disorders, memory function, and alcohol-related disorders. Its CAS number is 215874-86-5.
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| Molecular Formula |
C17H14N8O2
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|---|---|
| Molecular Weight |
362.35
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| Exact Mass |
362.124
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| CAS # |
215874-86-5
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| PubChem CID |
6918451
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| Appearance |
White to off-white solid powder
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| LogP |
1.948
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
527
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NZMJFRXKGUCYNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N8O2/c1-10-7-14(22-27-10)16-20-19-15-12-5-3-4-6-13(12)17(21-25(15)16)26-9-11-8-24(2)23-18-11/h3-8H,9H2,1-2H3
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| Chemical Name |
5-methyl-3-[6-[(1-methyltriazol-4-yl)methoxy]-[1,2,4]triazolo[3,4-a]phthalazin-3-yl]-1,2-oxazole
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| Synonyms |
L822179; L 822179; L-822179
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7598 mL | 13.7988 mL | 27.5976 mL | |
| 5 mM | 0.5520 mL | 2.7598 mL | 5.5195 mL | |
| 10 mM | 0.2760 mL | 1.3799 mL | 2.7598 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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