| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
L-701252 targets the glycine modulatory site of the N-methyl-D-aspartate (NMDA) receptor, a ligand-gated ion channel that plays a critical role in excitatory neurotransmission and synaptic plasticity. The NMDA receptor requires both glutamate and glycine (or D-serine) for activation. By binding to the glycine site, L-701252 acts as a competitive antagonist, preventing glycine from binding and thereby inhibiting NMDA receptor function. This mechanism of action distinguishes it from antagonists that target the glutamate-binding site.
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| ln Vitro |
In vitro, L-701252 is a potent antagonist of the glycine site of the NMDA receptor with an IC50 of 420 nM. Its activity is typically assessed in receptor binding assays or functional assays using cells expressing NMDA receptors. By blocking the glycine site, it inhibits NMDA receptor-mediated calcium influx and downstream signaling. Its selectivity for the glycine site over other NMDA receptor sites makes it a useful tool for dissecting the role of glycine in NMDA receptor function.
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| ln Vivo |
L-701252 (50 mg/kg; intraperitoneally) offered small but not significant protection [1].
In vivo, L-701252 has been evaluated for its neuroprotective properties. In a study using a model of global cerebral ischemia, administration of L-701252 at 50 mg/kg via intraperitoneal (i.p.) injection offered a small degree of neuroprotection. However, the protection was noted to be minimal and not statistically significant in some models. Despite its limited efficacy in this model, L-701252 remains a valuable tool for studying the role of the glycine site of the NMDA receptor in neurological conditions. |
| Enzyme Assay |
The inhibitory activity of L-701252 is assessed using in vitro receptor binding assays. Membranes from cells expressing NMDA receptors are incubated with a radiolabeled ligand specific for the glycine site (e.g., [³H]-MDL-105,519) and varying concentrations of L-701252. The bound and free radioligand are separated by filtration, and the radioactivity is measured. The IC50, the concentration required to inhibit 50% of specific binding, is calculated from competition curves.
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| Cell Assay |
The cellular activity of L-701252 is evaluated in cell lines expressing NMDA receptors, such as primary neuronal cultures or HEK293 cells transfected with NMDA receptor subunits. Cells are treated with L-701252 and then stimulated with NMDA and glycine. The compound's ability to inhibit NMDA receptor-mediated calcium influx is measured using calcium-sensitive fluorescent dyes. Its effect on downstream signaling, such as ERK phosphorylation, can also be assessed by Western blot.
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| Animal Protocol |
Animal/Disease Models: 3-month-old male Mongolian gerbil (60 g) [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Provided a small but insignificant protective effect. In animal studies, L-701252 is typically administered via intraperitoneal (i.p.) injection. In models of global cerebral ischemia, the compound is given prior to or after the ischemic event. Efficacy endpoints include the assessment of neuronal damage, infarct volume, and functional outcomes. Pharmacodynamic markers, such as NMDA receptor occupancy, can also be measured. |
| ADME/Pharmacokinetics |
Dosing regimens for L-701252 are determined based on its pharmacokinetic properties. It is soluble in DMSO (1.32 mg/mL) and is typically stored as a powder at -20°C. Its molecular weight is 263.68 g/mol, and its chemical formula is C13H10ClNO3. Detailed pharmacokinetic parameters, such as half-life and bioavailability, are not extensively documented in the provided sources.
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| Toxicity/Toxicokinetics |
Formal toxicology data for L-701252 is not extensively documented in the provided sources, as it is a research compound not intended for human therapeutic use. Its safety profile has not been established in comprehensive toxicology studies. However, its use in animal models at doses up to 50 mg/kg suggests it is tolerated in those contexts. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References |
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| Additional Infomation |
7-Chloro-3-[cyclopropyl(oxo)methyl]-4-hydroxy-1H-quinoline-2-one is a quinoline ketone and hydroxyquinoline.
L-701252 (CAS: 151057-13-5) is a well-characterized pharmacological tool for studying the glycine site of the NMDA receptor. Its IC50 of 420 nM makes it a useful compound for investigating the role of glycine in NMDA receptor function and for validating the glycine site as a therapeutic target. It has been cited in scientific literature for its potential in neuroprotection and is available from various commercial suppliers for research purposes. |
| Molecular Formula |
C13H10NO3CL
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|---|---|
| Molecular Weight |
263.6764
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| Exact Mass |
263.035
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| CAS # |
151057-13-5
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| PubChem CID |
54687453
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| Appearance |
White to off-white solid powder
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| Density |
1.573g/cm3
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| Boiling Point |
437.3ºC at 760mmHg
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| Flash Point |
218.3ºC
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| Vapour Pressure |
2.03E-08mmHg at 25°C
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| Index of Refraction |
1.694
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| LogP |
2.479
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
442
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MXEFWCFPCLDOOG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10ClNO3/c14-7-3-4-8-9(5-7)15-13(18)10(12(8)17)11(16)6-1-2-6/h3-6H,1-2H2,(H2,15,17,18)
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| Chemical Name |
7-chloro-3-(cyclopropanecarbonyl)-4-hydroxy-1H-quinolin-2-one
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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 : ~10 mg/mL (~37.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.79 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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7925 mL | 18.9624 mL | 37.9248 mL | |
| 5 mM | 0.7585 mL | 3.7925 mL | 7.5850 mL | |
| 10 mM | 0.3792 mL | 1.8962 mL | 3.7925 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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