An inhibitor of PDE2 and PDE3
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Carbazeran

Item No. 26092

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-ethyl-carbamic acid, 1-(6,7-dimethoxy-1-phthalazinyl)-4-piperidinyl ester
CAS Number
70724-25-3
Molecular Formula
C18H24N4O4
Formula Weight
360.4
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Chloroform: Slightly SolubleMethanol: Slightly Soluble
SMILES
COC1=C(OC)C=C(C=NN=C2N3CCC(OC(NCC)=O)CC3)C2=C1
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)
InChi Key
QJGVXJYGDBSPSJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $36

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    1 mg

    $68

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    5 mg

    $156

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    10 mg

    $268

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    Product Description

    Carbazeran is an inhibitor of phosphodiesterase 2 (PDE2) and PDE3.1 It inhibits cAMP hydrolysis (IC50 = 4.1 µM in rabbit heart ventricles) selectively over cGMP hydrolysis (IC50 = 171 µM).2 It induces positive inotropic (EC50 = 100 µM) and negative chronotropic effects in isolated rabbit papillary muscle and right atria, respectively. Carbazeran is also a substrate for the enzyme aldehyde oxidase (AOX1), which is involved in the metabolism of xenobiotics.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Price, B., Pyne, N.J., and Houslay, M.D. Proteolysis of cyclic AMP phosphodiesterase-II attenuates its ability to be inhibited by compounds which exert positive inotropic actions in cardiac tissue. Biochem. Pharmacol. 36(23), 4047-4054 (1987).

    2. Shahid, M., and Rodger, I.W. Chronotropic and inotropic actions of amrinone, carbazeran and isobutylmethyl xanthine: Role of phosphodiesterase inhibition. Br. J. Pharmacol. 98(1), 291-301 (1989).

    3. Hutzler, J.M., Yang, Y.S., Albaugh, D., et al. Characterization of aldehyde oxidase enzyme activity in cryopreserved human hepatocytes. Drug Metab. Dispos. 40(2), 267-275 (2012).

    4. Wilkinson, D.J., Southall, R.L., Li, M., et al. Minipig and human metabolism of aldehyde oxidase substrates: In Vitro-in Vivo comparisons. AAPS J. 19(4), 1163-1174 (2017).