4-Methylamino antipyrine

SKU: orb1940838

Description

4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak anti-inflammatory properties.(In Vitro):At room temperature and in an atmosphere with oxygen, Metamizole is spontaneously, nonenzymatically converted to 4-Methylamino antipyrine. Subsequently, the N-methyl side chain of 4-Methylamino antipyrine is oxidized to yield 4-formylaminoantipyrine, which is further converted to 4-aminoantipyrine .(In Vivo):Eight healthy male piglets are administered Metamizole (100 mg/kg) intramuscularly. 4-Methylamino antipyrine plasma concentrations are quantitatively detectable from 0.25 to 48 h. The average maximum concentration of 4-Methylamino antipyrine is 47.59 mg/mL. The average half-lives is 8.57 h for 4-Methylamino antipyrine .

Key Properties

• CAS Number: 519-98-2
• MW: 217.272
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₅N₃O
• SMILES: CNc1c(C)n(C)n(-c2ccccc2)c1=O
• Target: COX
• Solubility: In Vitro: DMSO : 50 mg/mL (230.13 mM)

Bioactivity

• In Vivo:
  The aim of this study is to assess the pharmacokinetics of its active metabolites 4-Methylamino antipyrine in male piglets after a single intramuscular injection of Metamizole. Eight healthy male piglets are administered Metamizole (100 mg/kg) intramuscularly. 4-Methylamino antipyrine plasma concentrations are quantitatively detectable from 0.25 to 48 h. The average maximum concentrations of 4-Methylamino antipyrine is of 47.59 mg/mL. The average half-lives is 8.57 h for 4-Methylamino antipyrine.
• In Vitro:
  Metamizole is a prodrug which, at room temperature and in an atmosphere with oxygen, is spontaneously, nonenzymatically converted to 4-Methylamino antipyrine. Subsequently, the N-methyl side chain of 4-Methylamino antipyrine is oxidized to yield 4-formylaminoantipyrine, which is further converted to 4-aminoantipyrine. Metamizole in aqueous solution and in the presence of oxygen consists of a group of several pyrazolone derivatives of which 4-Methylamino antipyrine is pharmacologically the most important.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

COX