| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
LQFM215 targets the L-proline transporter (PROT), also known as SLC6A7. It inhibits proline uptake by competitively binding to the active site of PROT. The compound also shows selectivity for cytochrome P450 isoforms, with a 10- to 16-fold selectivity for CYP3A4 over CYP3A5. This transporter and enzyme inhibition profile contributes to its neuroprotective and antipsychotic potential.
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| ln Vitro |
In vitro, LQFM215 inhibits proline uptake in hippocampal synaptosomes with an IC50 of 20.4 μM. It has been shown to have negligible neurotoxicity in LUHMES cells at pharmacologically active concentrations. The compound also demonstrates defined inhibition kinetics for CYP3A4 and CYP3A5. These activities validate its use as a probe for PROT function.
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| ln Vivo |
In vivo, LQFM215 (10.0 mg/kg) reduces animal motility without inducing anxious or depressive behaviors or cognitive impairments, as evaluated in the open-field test in mice. It prevents an increase in infarction area and motor impairments in the middle cerebral artery occlusion (MCAO) model of ischemic stroke. It also shows antipsychotic effects in a ketamine-induced psychosis model.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for LQFM215 typically involve measuring its inhibition of proline uptake. For example, hippocampal synaptosomes are incubated with 3H-proline and varying concentrations of LQFM215, and the amount of radiolabeled proline taken up is measured by scintillation counting. CYP inhibition assays are performed using standard probe substrates like midazolam and testosterone.
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| Cell Assay |
In vitro cell-based assay protocols for LQFM215 involve treating cultured cells, such as neuronal cell lines or primary neurons, with the compound to assess its effects on proline transport and cell viability. For neurotoxicity studies, LUHMES cells are treated with LQFM215, and cell viability is measured using standard assays like MTT.
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| Animal Protocol |
In vivo animal experimental protocols for LQFM215 have been established in mouse models. In the MCAO model of ischemic stroke, the compound is administered at 10 mg/kg to assess its neuroprotective effects by measuring infarct size and motor function. In models of psychosis, it is used to evaluate its antipsychotic potential. Behavioral tests like the open-field test are used to assess its effects on locomotion and anxiety.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LQFM215 are characterized by its solubility, with a solubility of 10 mM in DMSO. It has defined in vitro ADME data available for CYP inhibition profiling. Specific parameters such as half-life, Cmax, and oral bioavailability are not detailed in the available literature.
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| Toxicity/Toxicokinetics |
LQFM215 has been shown to have negligible neurotoxicity in LUHMES cells at pharmacologically active concentrations. It is not intended for human use and is strictly for research purposes. As a research chemical, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
LQFM215 is a research-grade compound used as a pharmacological tool to study the L-proline transporter (PROT) and its role in CNS disorders. It has shown efficacy in preclinical models of schizophrenia and ischemic stroke. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves inhibition of proline transport, and it is available exclusively for research purposes.
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| Molecular Formula |
C25H34N2O2
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|---|---|
| Molecular Weight |
394.55
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| Appearance |
White to off-white solid powder
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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 (~253.45 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5345 mL | 12.6727 mL | 25.3453 mL | |
| 5 mM | 0.5069 mL | 2.5345 mL | 5.0691 mL | |
| 10 mM | 0.2535 mL | 1.2673 mL | 2.5345 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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