PeptideDB

L-701252 151057-13-5

L-701252 151057-13-5

CAS No.: 151057-13-5

L-701252 is a potent glycine site NMDA receptor blocker (antagonist) with IC50 of 420 nM. L-701252 provides small-scale
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This product is for research use only, not for human use. We do not sell to patients.

L-701252 is a potent glycine site NMDA receptor blocker (antagonist) with IC50 of 420 nM. L-701252 provides small-scale neuroprotection against global cerebral ischemia.

Physicochemical Properties


Molecular Formula C13H10NO3CL
Molecular Weight 263.6764
Exact Mass 263.035
CAS # 151057-13-5
PubChem CID 54687453
Appearance White to off-white solid powder
Density 1.573g/cm3
Boiling Point 437.3ºC at 760mmHg
Flash Point 218.3ºC
Vapour Pressure 2.03E-08mmHg at 25°C
Index of Refraction 1.694
LogP 2.479
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 2
Heavy Atom Count 18
Complexity 442
Defined Atom Stereocenter Count 0
InChi Key MXEFWCFPCLDOOG-UHFFFAOYSA-N
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)
Chemical Name

7-chloro-3-(cyclopropanecarbonyl)-4-hydroxy-1H-quinolin-2-one
HS Tariff Code 2934.99.9001
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)

Biological Activity


ln Vivo L-701252 (50 mg/kg; intraperitoneally) offered small but not significant protection [1].
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.
References

[1]. Stone TW. Development and therapeutic potential of kynurenic acid and kynurenine derivatives for neuroprotection. Trends Pharmacol Sci. 2000;21(4):149-154.

[2]. Failure of glycine site NMDA receptor antagonists to protect against L-2-chloropropionic acid-induced neurotoxicity highlights the uniqueness of cerebellar NMDA receptors. Brain Res. 1996;738(2):236-242.

Additional Infomation 7-chloro-3-[cyclopropyl(oxo)methyl]-4-hydroxy-1H-quinolin-2-one is a quinolone and a hydroxyquinoline.

Solubility Data


Solubility (In Vitro) DMSO : ~10 mg/mL (~37.92 mM)
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.