| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
The primary molecular target of LAU159 is the GABA(A) receptor, specifically the α1β3 subtype. GABA(A) receptors are ligand-gated ion channels that mediate inhibitory neurotransmission in the central nervous system. LAU159 acts as a functionally selective positive modulator of the α1β3 GABA(A) receptor with an EC50 of 2.2 μM. It is also a positive allosteric modulator (PAM) of α6β3γ2 subunit-containing GABAA receptors. The compound selectively increases GABA-induced currents in X. laevis oocytes expressing α6β3γ2 over other subunit-containing receptors at 10 μM. This functional selectivity makes LAU159 a valuable tool for studying GABA(A) receptor subtype-specific pharmacology.
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| ln Vitro |
In vitro studies demonstrate that LAU159 is a functionally selective positive modulator of the α1β3 GABA(A) receptor with an EC50 of 2.2 μM. It selectively increases GABA-induced currents in X. laevis oocytes expressing α6β3γ2 over α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, and α5β3γ2 subunit-containing receptors at 10 μM. The compound's positive allosteric modulation enhances the response of the receptor to GABA, the endogenous neurotransmitter. This activity makes LAU159 a valuable tool for studying GABA(A) receptor pharmacology and for investigating the role of specific receptor subtypes in neurological function and disease.
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| ln Vivo |
In vivo studies of LAU159 are limited, as the compound is primarily used as a research reagent. Its ability to modulate GABA(A) receptor activity suggests potential applications in studying neurological disorders such as anxiety, epilepsy, and sleep disorders. However, no extensive in vivo pharmacological or toxicological studies have been reported. The compound is used for research purposes only and is not intended for therapeutic use.
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| Enzyme Assay |
For GABA(A) receptor functional assays, Xenopus laevis oocytes are injected with cRNA encoding the desired GABA(A) receptor subunits (e.g., α1, β3, and γ2). After 2-5 days of incubation, oocytes are placed in a recording chamber and perfused with Ringer's solution. Two-electrode voltage clamp (TEVC) is used to measure GABA-induced currents. LAU159 is dissolved in DMSO and diluted in Ringer's solution to final concentrations (typically 0.001-100 µM). Oocytes are first perfused with GABA alone to establish baseline currents, then with GABA plus LAU159 to assess modulation. The potentiation of GABA-induced currents is calculated as the percentage increase over baseline. EC50 values are calculated from dose-response curves.
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| Cell Assay |
For cellular studies, cell lines expressing GABA(A) receptors (e.g., HEK-293 cells transfected with receptor subunits) can be used. Cells are cultured in appropriate medium and seeded in 96-well plates. LAU159 is dissolved in DMSO and diluted in culture medium to final concentrations (typically 0.001-100 µM). For calcium flux assays, cells are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM) and stimulated with GABA in the presence or absence of LAU159. Fluorescence is measured using a fluorescence plate reader. For electrophysiology studies, patch-clamp recordings are performed on cells expressing GABA(A) receptors to measure the effect of LAU159 on GABA-induced currents.
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| Animal Protocol |
For in vivo studies, adult mice or rats may be used to evaluate the effects of LAU159 on behavior and neurological function. The compound would be administered intraperitoneally or orally at doses determined from preliminary studies. Behavioral tests such as the elevated plus maze, open field test, and seizure models could be used to assess anxiolytic, sedative, or anticonvulsant effects. However, no specific in vivo protocols have been reported for LAU159.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for LAU159 are limited, as the compound is a research tool. As a small-molecule with a molecular weight of 325.75, the compound is expected to have moderate oral bioavailability and tissue distribution. Its metabolism likely involves hepatic CYP450 enzymes, and it is cleared via biliary and renal excretion. However, no dedicated pharmacokinetic studies have been reported. The compound is primarily used in vitro and is not intended for in vivo pharmacokinetic characterization.
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| Toxicity/Toxicokinetics |
Toxicological data for LAU159 are limited, as the compound is used as a research reagent. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research compounds, appropriate safety precautions should be taken when handling LAU159, including the use of personal protective equipment and work in a well-ventilated area.
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| References |
: Varagic Z, et al. Identification of novel positive allosteric modulators and null modulators at the GABAA receptor α+β- interface. Br J Pharmacol. 2013 May;169(2):371-83.
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| Additional Infomation |
LAU159 (CAS 2055050-87-6) is a pyrazoloquinolinone-derived research compound. It has a molecular formula of C₁₇H₁₂ClN₃O₂ and a molecular weight of 325.75. LAU159 is a functionally selective positive modulator of the α1β3 GABA(A) receptor with an EC50 of 2.2 μM. It is also a PAM of α6β3γ2 subunit-containing GABAA receptors. The compound selectively increases GABA-induced currents in X. laevis oocytes expressing α6β3γ2 over other subtypes at 10 μM. LAU159 is a valuable tool for studying GABA(A) receptor pharmacology and is strictly for research use only.
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| Molecular Formula |
C₁₇H₁₂CLN₃O₂
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| Molecular Weight |
325.75
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| Exact Mass |
325.061
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| CAS # |
2055050-87-6
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| PubChem CID |
124111373
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
473.8±55.0 °C at 760 mmHg
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| Flash Point |
240.3±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.706
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| LogP |
3.16
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
463
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2=C(C=C(Cl)C=C2)C2=NN(C3=CC=CC(OC)=C3)C(=O)C2=C1
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| InChi Key |
WQYIIWQWPXNTAK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12ClN3O2/c1-23-12-4-2-3-11(8-12)21-17(22)14-9-19-15-6-5-10(18)7-13(15)16(14)20-21/h2-9,19H,1H3
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| Chemical Name |
8-chloro-2,5-dihydro-2-(3-methoxyphenyl)-3H-pyrazolo[4,3-c]quinolin-3-one
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| Synonyms |
LAU159 LAU-159 LAU 159
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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 |
| 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 | 3.0698 mL | 15.3492 mL | 30.6984 mL | |
| 5 mM | 0.6140 mL | 3.0698 mL | 6.1397 mL | |
| 10 mM | 0.3070 mL | 1.5349 mL | 3.0698 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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