Carbazeran | CAS#70724-25-3 | PDE-II Inhibitor

MedKoo Cat#: 524551 | Name: Carbazeran

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Description:

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

Carbazeran is an Aldehyde oxidase (AO) substrate and potent phosphodiesterase PDE-II and PDE-III inhibitor that produces concentration-dependent positive inotropic responses. Carbazeran shows chronotropic and inotropic effect in vivo (EC50 = 100 μM, ionotropic effects, independent of adrenergic mechanisms). It potently inhibits cAMP hydrolysis. In humans, the compound is almost completely cleared via 4-hydroxylation to the phthalazinone metabolite by AO.

Chemical Structure

Carbazeran

CAS#70724-25-3

Theoretical Analysis

MedKoo Cat#: 524551

Name: Carbazeran

CAS#: 70724-25-3

Chemical Formula: C18H24N4O4

Exact Mass: 360.1798

Molecular Weight: 360.41

Elemental Analysis: C, 59.99; H, 6.71; N, 15.55; O, 17.76

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 650.00	2 Weeks
50mg	USD 950.00	2 Weeks

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Related CAS #

No Data

Synonym

Carbazeran; UK 31557; UK-31557; UK31557; UK 31,557; UK-31,557; UK31,557.

IUPAC/Chemical Name

1-(6,7-dimethoxyphthalazin-1-yl)piperidin-4-yl ethylcarbamate

InChi Key

QJGVXJYGDBSPSJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H24N4O4/c1-4-19-18(23)26-13-5-7-22(8-6-13)17-14-10-16(25-3)15(24-2)9-12(14)11-20-21-17/h9-11,13H,4-8H2,1-3H3,(H,19,23)

SMILES Code

c1(c(OC)cc2c(c1)c(nnc2)N1CCC(CC1)OC(NCC)=O)OC

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, not in water

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 360.41 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.

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

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Genetic variants of aldehyde oxidase (AOX) 1 in cynomolgus and rhesus macaques. Xenobiotica. 2021 Apr;51(4):494-499. doi: 10.1080/00498254.2021.1874564. Epub 2021 Jan 17. PMID: 33434089. 9: Taylor CR, Baird JR, Blackburn KJ, Cambridge D, Constantine JW, Ghaly MS, Hayden ML, McIlhenny HM, Moore PF, Olukotun AY, Pullman LG, Salsburg DS, Saxton CA, Shevde S. Comparative pharmacology and clinical efficacy of newer agents in treatment of heart failure. Am Heart J. 1981 Sep;102(3 Pt 2):515-32. doi: 10.1016/0002-8703(81)90740-7. PMID: 7023221. 10: Kato S, Shah A, Plesescu M, Miyata Y, Bolleddula J, Chowdhury S, Zhu X. Prediction of Human Disproportionate and Biliary Excreted Metabolites Using Chimeric Mice with Humanized Liver. Drug Metab Dispos. 2020 Oct;48(10):934-943. doi: 10.1124/dmd.120.000128. Epub 2020 Jul 14. PMID: 32665417. 11: Hoey M, Houslay MD. Identification and selective inhibition of four distinct soluble forms of cyclic nucleotide phosphodiesterase activity from kidney. 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PMID: 3130251. 19: Sharma R, Strelevitz TJ, Gao H, Clark AJ, Schildknegt K, Obach RS, Ripp SL, Spracklin DK, Tremaine LM, Vaz AD. Deuterium isotope effects on drug pharmacokinetics. I. System-dependent effects of specific deuteration with aldehyde oxidase cleared drugs. Drug Metab Dispos. 2012 Mar;40(3):625-34. doi: 10.1124/dmd.111.042770. Epub 2011 Dec 21. PMID: 22190693. 20: Tan WK, Tan ARY, Sivanandam P, Goh EJH, Yap ZP, Saburulla NF, Austin-Muttitt K, Mullins JGL, Lau AJ. In Vitro Inhibition of Human Aldehyde Oxidase Activity by Clinically Relevant Concentrations of Gefitinib and Erlotinib: Comparison with Select Metabolites, Molecular Docking Analysis, and Impact on Hepatic Metabolism of Zaleplon and Methotrexate. J Pharmacol Exp Ther. 2020 Aug;374(2):295-307. doi: 10.1124/jpet.120.265249. Epub 2020 May 11. PMID: 32393528.