MedKoo Cat#: 412917 | Name: Apazone (free base)

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Apazone (free base) is a non-steroidal anti-inflammatory drug. It is indicated for use in the treatment of rheumatoid arthritis, osteo-arthritis and gout. Gastro-intestinal disturbances, allergic skin rashes and photosensitivity, headache, vertigo, oedema and kidney impairment may occur. Gastro-intestinal bleeding and angioedema have been reported. Pre-treatment with this drug failed to modify plasma concentrations of phenobarbitone. Brain levels of imipramine or desmethyl imipramine were unaffected 60 minutes after oral administration of imipramine.

Chemical Structure

Apazone (free base)
Apazone (free base)
CAS#13539-59-8 (free base)

Theoretical Analysis

MedKoo Cat#: 412917

Name: Apazone (free base)

CAS#: 13539-59-8 (free base)

Chemical Formula: C16H20N4O2

Exact Mass: 300.1586

Molecular Weight: 300.36

Elemental Analysis: C, 63.98; H, 6.71; N, 18.65; O, 10.65

Price and Availability

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Synonym
Azapropazone; Apazone; AHR-3018; DuP-141; MI-85; NSC-102824; AHR 3018; DuP 141; MI 85; NSC 102824; AHR3018; DuP141; MI85; NSC102824; Rheumox
IUPAC/Chemical Name
1H-Pyrazolo(1,2-a)(1,2,4)benzotriazine-1,3(2H)-dione, 5-(dimethylamino)-9-methyl-2-propyl-
InChi Key
MPHPHYZQRGLTBO-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H20N4O2/c1-5-6-11-14(21)19-13-9-10(2)7-8-12(13)17-16(18(3)4)20(19)15(11)22/h7-9,11H,5-6H2,1-4H3
SMILES Code
O=C(N1N2C(N(C)C)=NC3=CC=C(C)C=C31)C(CCC)C2=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 300.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Apazone. 2020 Jul 20. PMID: 29999744. 2: Steffen P, Wiedemann S, Georgieff M, Hähnel J, Treiber H, Seeling W. Kombinierte intravenöse Gabe von Diclofenac und Azapropazon zur postoperativen Analgesie : Eine randomisierte Doppelblindstudie an 112 unfallchirurgischen Patienten mittels der intravenösen On-Demand-Analgesie [Combined intravenous administration of diclofenac and apazone for postoperative analgesia A randomized study of 112 patients with access to i. v. on-demand analgesia after minor orthopaedic operations.]. Schmerz. 1994 Dec;8(4):235-42. German. doi: 10.1007/BF02527892. PMID: 18415463. 3: Urien S, Albengres E, Pinquier JL, Tillement JP. Role of alpha-1 acid glycoprotein, albumin, and nonesterified fatty acids in serum binding of apazone and warfarin. Clin Pharmacol Ther. 1986 Jun;39(6):683-9. doi: 10.1038/clpt.1986.119. PMID: 3709033. 4: Johnson AG, Day RO. The problems and pitfalls of NSAID therapy in the elderly (Part I). Drugs Aging. 1991 Mar;1(2):130-43. doi: 10.2165/00002512-199101020-00005. PMID: 1794009. 5: Huskisson EC. Antiinflammatory drugs. Semin Arthritis Rheum. 1977 Aug;7(1):1-20. doi: 10.1016/s0049-0172(77)80002-4. PMID: 20668. 6: Bree F, Nguyen P, Urien S, Riant P, Albengres E, Fenner H, Tillement JP. Blood distribution of tenoxicam in humans: a particular HSA drug interaction. Fundam Clin Pharmacol. 1989;3(3):267-79. doi: 10.1111/j.1472-8206.1989.tb00456.x. PMID: 2767607. 7: Jones CJ. The pharmacology and pharmacokinetics of azapropazone - a review. Curr Med Res Opin. 1976;4(1):3-16. doi: 10.1185/03007997609109277. PMID: 770078. 8: Saenz A, Ausejo M, Shea B, Wells G, Welch V, Tugwell P. Pharmacotherapy for Behcet's syndrome. Cochrane Database Syst Rev. 2000;1998(2):CD001084. doi: 10.1002/14651858.CD001084. PMID: 10796413; PMCID: PMC7032645. 9: Brée F, Urien S, Nguyen P, Riant P, Albengres E, Tillement JP. A re- evaluation of the HSA-piroxicam interaction. Eur J Drug Metab Pharmacokinet. 1990 Oct-Dec;15(4):303-7. doi: 10.1007/BF03190219. PMID: 2088766. 10: Brooks PM, Buchanan WW. Azapropazone - its place in the management of rheumatoid conditions. Curr Med Res Opin. 1976;4(1):94-100. doi: 10.1185/03007997609109288. PMID: 770085.