| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
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| ln Vitro |
Metamizole sodium hydrate (1 and 10 μM, 24 h) suppresses osteoblast development, which lowers the osteoblasts' capacity to create new extracellular matrix that mineralizes bone [2]. In the pancreatic cancer cell lines PaTu 8988 t and Panc-1, metamizole sodium hydrate (1-500 μM, 48 h) can increase cell death and limit cell growth [3].
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| ln Vivo |
Rats treated with 500 mg/kg of metamizole sodium hydrate intraperitoneally twice a day for seven days will show less signs of developing neuropathic pain [4]. In rats, oxidative stress brought on by incision and carrageenan can be successfully reduced by oral administration of metamizole sodium hydrate (250 or 500 mg/kg) [5].
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| Cell Assay |
Cell Proliferation Assay[3]
Cell Types: PaTu 8988 t, Panc-1 Tested Concentrations: 1, 10, 100, 250, 500 μM Incubation Duration: 48 h Experimental Results: Inhibited proliferation in the PaTu 8988 t cell line with 1–500 μM and with concentrations of 1 μM, 10 μM, 100 μM, and 250 μM in the Panc-1 cell line. Increased the apoptosis rate after 9 h. |
| Animal Protocol |
Animal/Disease Models: Neuropathic pain rat model [4]
Doses: 500 mg/kg Route of Administration: intraperitoneally preemptively at 16 and 1 h before Chronic constriction injury (CCI) and then twice a day for 7 days. Experimental Results: diminished the expression of pronociceptive interleukins ( IL-1beta, IL-6, and IL-18) and chemokines (CCL2, CCL4, and CCL7). Animal/Disease Models: Pain model in rats [5] Doses: 250 or 500 mg/kg Route of Administration: po Experimental Results: diminished the COX -2 gene expression at 500 mg/kg and increased the MPO gene expression. decreased MDA levels in the carrageenan paw test and increased tGSH levels. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation After ingestion by the mother, dipyrone and its metabolites appear in breastmilk in rather large amounts. It is found in the blood and urine of breastfed infants and can cause pharmacological effects in the breastfed infant. One case of cyanotic episodes in a breastfed infant was attributed to dipyrone in breastmilk. The drug and metabolites are eliminated from the breastmilk by 48 hours after a dose. Dipyrone is not approved for marketing in the United States by the U.S. Food and Drug Administration nor in Canada and many European countries because of its adverse reactions, including agranulocytosis. However, it is widely used in other countries during labor and breastfeeding. The European Medicines Agency recommends that dipyrone not be used in nursing mothers; however, several drug consultation centers in Israel disagree. One manufacturer recommends to withhold breastfeeding for 48 hours after a dose. Safer alternatives are available for analgesia during breastfeeding. ◉ Effects in Breastfed Infants A 42-day-old breastfed infant had 2 cyanotic episodes within 30 minutes after his mother took 3 doses of dipyrone 500 mg orally, 18, 7 and 2 hours before the first episode. A third episode occurred 24 hours after admission to the hospital. Dipyrone was detected in the mother's breastmilk 24 hours after the last dose and in the infant's serum and urine. No explanation could be found for the cyanotic episodes other than dipyrone and after suspending maternal dipyrone intake, no further episodes occurred in the infant up to age 3 years. The reaction is rated as possibly caused by dipyrone in breastmilk. In a blinded study, mothers who were at least 3 days postpartum and requesting analgesia for postpartum uterine pain were given either 1 gram of dipyrone or placebo. The infants of mothers who received dipyrone cried fewer times and for shorter durations in the 14 hours after drug administration than the infants of mothers who received placebo. This effect was more apparent in infants who demand fed than in those who fed on a fixed schedule. Although this study appears to demonstrate a pharmacologic effect in the infants from dipyrone in milk, there is no clear explanation for the change in infant behavior. A multicenter case-control study in Brazil compared 231 children who developed leukemia before 2 years of age with 411 children with various other nonmalignant diseases. Mothers were interviewed to ascertain their analgesic use during pregnancy and lactation. Nursing mothers who took dipyrone during the three months after delivery had a 2-fold risk of having a child with acute lymphocytic leukemia and a 3.87-fold risk in having rearrangement of the MLL gene in infants under one year of age. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References | |
| Additional Infomation |
Metamizole sodium is an organic sodium salt of antipyrine substituted at C-4 by a methyl(sulfonatomethyl)amino group, commonly used as a powerful analgesic and antipyretic. It has a role as a non-narcotic analgesic, an antirheumatic drug, a peripheral nervous system drug, an antipyretic, a prodrug, a cyclooxygenase 3 inhibitor and an anti-inflammatory agent. It contains a metamizole(1-).
A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE. |
| Molecular Formula |
C13H18N3NAO5S
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|---|---|
| Molecular Weight |
351.3528
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| Exact Mass |
333.075
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| CAS # |
5907-38-0
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| Related CAS # |
Metamizole sodium;68-89-3
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| PubChem CID |
522325
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| Appearance |
White to off-white solid powder
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| LogP |
1.504
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
552
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DJGAAPFSPWAYTJ-UHFFFAOYSA-M
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| 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
|
| Chemical Name |
sodium;[(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)-methylamino]methanesulfonate
|
| Synonyms |
NSC 73205; NSC-73205; Dipyrone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~284.62 mM)
H2O : ≥ 100 mg/mL (~284.62 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 100 mg/mL (284.62 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8462 mL | 14.2308 mL | 28.4616 mL | |
| 5 mM | 0.5692 mL | 2.8462 mL | 5.6923 mL | |
| 10 mM | 0.2846 mL | 1.4231 mL | 2.8462 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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