Carbazeran citrate
Carbazeran citrate is a phosphodiesterase inhibitor. Carbazeran citrate is oxidized by aldehyde oxidase/AOX1 to 4-oxo-Carbazeran citrate/hydroxyCarbazeran citrate, serving as an AOX1 probe and competitively inhibiting xanthine oxidase. Carbazeran citrate can be used in research on congestive heart failure and chronic heart failure.
For research use only. We do not sell to patients.
- CAS No.: 153473-94-0
- Formula: C24H32N4O11
- Molecular Weight:552.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Carbazeran citrate selectively inhibits rat kidney cytosol cyclic AMP-specific KPDE-MQ-V and KPDE-MQ-IV with Ki values of 6-8.0 μM[1].
Carbazeran citrate weakly inhibits bovine retinal cyclic GMP-specific phosphodiesterase with a Ki of 168 μM[1].
Carbazeran citrate is a high-affinity substrate for guinea-pig and baboon liver aldehyde oxidase (Km 0.053 and 0.009 mM, respectively) and a competitive inhibitor of bovine milk xanthine oxidase (Ki 0.015 mM), with no interaction with rabbit liver aldehyde oxidase[2].
Carbazeran citrate inhibits isolated cyclic AMP phosphodiesterase with an IC50 of 17.5 μM[7].
Carbazeran citrate does not demonstrably inhibit cardiac Na+,K+-ATPase activity[7].
Carbazeran citrate increases cyclic AMP levels in rabbit right ventricular papillary muscles[7].
Carbazeran citrate (4-20 mM extracellular K+) restores contractility in potassium-depolarized rabbit papillary muscles[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 153473-94-0
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Molecular Weight 552.53
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Formula C24H32N4O11
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SMILES
O=C(OC1CCN(C2=NN=CC3=C2C=C(OC)C(OC)=C3)CC1)NCC.O=C(CC(C(O)=O)(O)CC(O)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
References
[1]. Hoey M, et al. Identification and selective inhibition of four distinct soluble forms of cyclic nucleotide phosphodiesterase activity from kidney. Biochemical pharmacology. 1990 Jul 15;40(2):193-202. [Content Brief]
[3]. Fu C, et al. Aldehyde oxidase 1 (AOX1) in human liver cytosols: quantitative characterization of AOX1 expression level and activity relationship. Drug metabolism and disposition: the biological fate of chemicals. 2013 Oct;41(10):1797-804. [Content Brief]
[9]. Uehara S, et al. Human Aldehyde Oxidase 1-Mediated Carbazeran Oxidation in Chimeric TK-NOG Mice Transplanted with Human Hepatocytes. Drug metabolism and disposition: the biological fate of chemicals. 2020 Jul;48(7):580-586. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Carbazeran citrate Related Classifications
HY-108680 Related Classifications
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