Metamizole-d3 (sodium salt)

Metamizole-d3 is intended for use as an internal standard for the quantification of metamizole (Cay-15771) by GC- or LC-MS. Metamizole is a nonopioid prodrug that is rapidly hydrolyzed to the analgesic and antipyretic metabolites 4-methylaminoantipyrine (MAA) and 4-aminoantipyrine (AA). 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). Metamizole (6, 12, and 25 µg/ml) inhibits ADP- and epinephrine-induced platelet aggregation in human platelet-rich plasma (hPRP). It prevents fever induced by LPS, TNF-alpha, and IL-6, but not arachidonic acid (Cay-90010, Cay-90010.1, Cay-10006607) or prostaglandin E2 (PGE2, Cay-14010), in rats when administered at a dose of 120 mg/kg. 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.Formal Name: ((1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)(methyl-d3)amino)methanesulfonate, monosodium salt. CAS Number: 2512223-60-6. Synonyms: Dipyrone-d3. Molecular Formula: C13H13D3N3O4S . Na. Formula Weight: 336.4. Purity: >99% deuterated forms (d1-d3). Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble, Methanol: soluble. SMILES: [O-]S(CN(C([2H])([2H])[2H])C1=C(C)N(C)N(C2=CC=CC=C2)C1=O)(=O)=O.[Na+]. InChi Code: InChI=1S/C13H17N3O4S.Na/c1-10-12(14(2)9-21(18,19)20)13(17)16(15(10)3)11-7-5-4-6-8-11,/h4-8H,9H2,1-3H3,(H,18,19,20),/q,+1/p-1/i2D3,. InChi Key: DJGAAPFSPWAYTJ-MUTAZJQDSA-M. Origin: Synthetic.