A nonopioid prodrug; inhibits COX-1 and COX-2 activity (IC50 = ~150 µg/ml for both in cell-free assays)

Metamizole (sodium salt) – 50 g

Brand:
Cayman
CAS:
68-89-3
Storage:
-20
UN-No:
Non-Hazardous - /

Metamizole is a nonopioid prodrug that is rapidly hydrolyzed to the analgesic and antipyretic metabolites 4-methylaminoantipyrine (MAA) and 4-aminoantipyrine (AA).{25749} It inhibits COX-1 and COX-2 activity (IC50 = ~150 µg/ml for both in cell-free assays), as well as reduces increases in intracellular calcium levels induced by the TRPA1 agonist AITC in isolated rat and mouse dorsal root ganglia and IMR-90 human fibroblasts (IC50s = 30-91 µM in patch-clamp assays).{46639,46640} Metamizole (6, 12, and 25 µg/ml) inhibits ADP- and epinephrine-induced platelet aggregation in human platelet-rich plasma (hPRP).{46641} It prevents fever induced by LPS, TNF-α, and IL-6, but not arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) or prostaglandin E2 (PGE2; Item No. 14010), in rats when administered at a dose of 120 mg/kg.{46642} Metamizole (250 and 500 mg/kg) increases the paw withdrawal threshold in the paw pressure test, indicating analgesic activity, in rat models of carrageenan-induced acute pain and postoperative incision pain.{46643}  

 

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Description

A nonopioid prodrug; inhibits COX-1 and COX-2 activity (IC50 = ~150 µg/ml for both in cell-free assays), as well as reduces AITC-induced increases in intracellular calcium levels in isolated rat and mouse dorsal root ganglia and IMR-90 human fibroblasts (IC50s = 30-91 µM in patch-clamp assays); inhibits ADP- and epinephrine-induced platelet aggregation in hPRP; prevents fever induced by LPS, TNF-α, and IL-6, but not arachidonic acid or PGE2, in rats at 120 mg/kg; increases the paw withdrawal threshold in the paw pressure test in rat models of carrageenan-induced acute pain and postoperative incision pain at 250 and 500 mg/kg

Formal name: 1-[(2,3-dihydro-1,5-dimethyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)methylamino]-methanesulfonic acid, monosodium salt

Synonyms:  Dipyrone

Molecular weight: 333.3

CAS: 68-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Cyclooxygenases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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