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AS057278

Cat. No. M20487
AS057278 Structure
Synonym:

3-Methylpyrazole-5-carboxylic acid

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Biological Activity

AS057278 (3-Methylpyrazole-5-carboxylic acid, MPC) is an inhibitor of D-amino acid oxidase (DAAO).

Chemical Information
Molecular Weight 126.11
Formula C5H6N2O2
CAS Number 402-61-9
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nian Gong, et al. Anesthesiology. Identification of a novel spinal dorsal horn astroglial D-amino acid oxidase-hydrogen peroxide pathway involved in morphine antinociceptive tolerance

[2] Nian Gong, et al. J Pharmacol Exp Ther. A series of D-amino acid oxidase inhibitors specifically prevents and reverses formalin-induced tonic pain in rats

[3] Tadahiro Ogaya, et al. Neurochem Res. Changes in extracellular kynurenic acid concentrations in rat prefrontal cortex after D-kynurenine infusion: an in vivo microdialysis study

[4] Michael Williams. Biochem Pharmacol. Commentary: genome-based CNS drug discovery: D-amino acid oxidase (DAAO) as a novel target for antipsychotic medications: progress and challenges

[5] Tiziana Adage, et al. Eur Neuropsychopharmacol. In vitro and in vivo pharmacological profile of AS057278, a selective d-amino acid oxidase inhibitor with potential anti-psychotic properties

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Keywords: AS057278, 3-Methylpyrazole-5-carboxylic acid supplier, inhibitors, activators

 
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