1. Immunology/Inflammation
    Metabolic Enzyme/Protease
  2. COX
    Drug Metabolite
  3. 4-Methylamino antipyrine

4-Methylamino antipyrine 

Cat. No.: HY-135731 Purity: ≥98.0%
Handling Instructions

4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.

For research use only. We do not sell to patients.

4-Methylamino antipyrine Chemical Structure

4-Methylamino antipyrine Chemical Structure

CAS No. : 519-98-2

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25 mg USD 105 In-stock
Estimated Time of Arrival: December 31
50 mg USD 155 In-stock
Estimated Time of Arrival: December 31
100 mg USD 245 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever[1][2][3]. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties[2].

IC50 & Target
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

217.27

Formula

C₁₂H₁₅N₃O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (230.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.6026 mL 23.0128 mL 46.0257 mL
5 mM 0.9205 mL 4.6026 mL 9.2051 mL
10 mM 0.4603 mL 2.3013 mL 4.6026 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (11.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
4-Methylamino antipyrine
Cat. No.:
HY-135731
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