| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Lorediplon targets the GABAA receptor, specifically the α1 subunit. By binding to this subunit, it enhances the effect of GABA on GABAA receptors, leading to increased chloride ion influx and neuronal hyperpolarization.
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| ln Vitro |
In vitro, lorediplon acts as a selective modulator of the GABAA receptor, particularly targeting the α1 subunit. It differentially modulates GABAA receptor activity.
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| ln Vivo |
In vivo, lorediplon inhibits spontaneous motor activity and increases duration of sleep in mice (ED50s = 0.13 and 1.2 mg/kg, respectively). It selectively inhibits spontaneous motor activity driven by α1 subunit-containing GABAA receptors over modification of muscular tone driven by α2 subunit-containing receptors. It decreases latency to slow wave sleep (SWS) and paradoxical sleep (PS) in mice.
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| Enzyme Assay |
In vitro receptor binding assays measure the displacement of a radiolabeled GABAA receptor ligand from brain membrane preparations. Lorediplon is incubated with membranes and a radioactive tracer, and the IC50 or Ki is determined. Selectivity for the α1 subunit is assessed using recombinant receptors.
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| Cell Assay |
In vitro cellular assays evaluate the modulatory effects of lorediplon on GABAA receptors using electrophysiological techniques such as patch-clamp recordings. Cells expressing GABAA receptors are treated with the compound, and chloride currents are measured in the presence of GABA.
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| Animal Protocol |
In vivo animal experiments are conducted in mice to evaluate the sedative and hypnotic effects of lorediplon. The compound is administered orally or intraperitoneally, and spontaneous motor activity, sleep duration, and latency to sleep are measured.
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| ADME/Pharmacokinetics |
Lorediplon has a molecular formula of C20H15FN4O2S and a molecular weight of 394.42. It has a CAS number of 917393-39-6. After oral administration, it is rapidly absorbed, reaching maximum plasma concentrations at approximately 2 hours. It is mainly metabolized through CYP3A4.
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| Toxicity/Toxicokinetics |
The toxicity profile of lorediplon is consistent with that of other GABAA receptor modulators. No next-day hangover effects were observed in studies. The compound demonstrated a dose-dependent improvement in sleep.
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| References |
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| Additional Infomation |
Lorediplon is a hypnotic drug being developed for the treatment of insomnia. It is a non-benzodiazepine of the pyrazolopyrimidine family. It has not completed development. Clinical trials in patients with insomnia have been warranted.
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| Molecular Formula |
C20H15FN4O2S
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|---|---|
| Molecular Weight |
394.42
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| Exact Mass |
394.09
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| CAS # |
917393-39-6
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| Related CAS # |
917393-39-6;
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| PubChem CID |
12004146
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.81
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
609
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NQPOCLFSADOXBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15FN4O2S/c1-12(26)24(2)17-10-13(5-6-15(17)21)16-7-8-22-20-14(11-23-25(16)20)19(27)18-4-3-9-28-18/h3-11H,1-2H3
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| Chemical Name |
N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide
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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) |
DMSO : ~100 mg/mL (~253.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5354 mL | 12.6768 mL | 25.3537 mL | |
| 5 mM | 0.5071 mL | 2.5354 mL | 5.0707 mL | |
| 10 mM | 0.2535 mL | 1.2677 mL | 2.5354 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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