An inhibitor of PDE4
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E6005

Item No. 30203

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[[3-[6,7-dimethoxy-2-(methylamino)-4-quinazolinyl]phenyl]amino]carbonyl]-benzoic acid, methyl ester
CAS Number
947620-48-6
Synonyms
  • RVT-501
Molecular Formula
C26H24N4O5
Formula Weight
472.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 1mg/mLDMSO:PBS (pH 7.2) (1:2): 0.3mg/mL
SMILES
O=C(OC)C1=CC=C(C(NC2=CC(C3=NC(NC)=NC4=C3C=C(OC)C(OC)=C4)=CC=C2)=O)C=C1
InChi Code
InChI=1S/C26H24N4O5/c1-27-26-29-20-14-22(34-3)21(33-2)13-19(20)23(30-26)17-6-5-7-18(12-17)28-24(31)15-8-10-16(11-9-15)25(32)35-4/h5-14H,1-4H3,(H,28,31)(H,27,29,30)
InChi Key
BBTFKAOFCSOZMB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    E6005 is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2.8 nM).1 It is selective for PDE4 over PDE1, PDE2, PDE3, and PDE5 with only 46.1, 51.6, 69.4, and 57.4% inhibition, respectively, at 30 µM. It inhibits the production of various cytokines in isolated human lymphocytes and monocytes (IC50s = 0.49-3.1 nM). Topical application of E6005 (0.003-0.3%) reduces ear thickness in a mouse model of oxazolone-induced skin inflammation, as well as reduces oxazolone-induced scratching in mice. It reduces the severity of skin lesions in a model of mite-induced atopic dermatitis. Topical application of E6005 (0.03%) also inhibits the production of leukotriene B4 (LTB4; Item No. 20110) in mouse skin, as well as reduces scratching and cutaneous nerve firing induced by the proteinase-activated receptor 2 (PAR2) agonist SLIGRL-NH2 (Item No. 16723) in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ishii, N., Shirato, M., Wakita, H., et al. Antipruritic effect of the topical phosphodiesterase 4 inhibitor E6005 ameliorates skin lesions in a mouse atopic dermatitis mode. J. Pharmacol. Exp. Ther. 346(1), 105-112 (2013).

    2. Andoh, T., and Kuraishi, Y. Antipruritic mechanisms of topical E6005, a phosphodiesterase 4 inhibitor: Inhibition of responses to proteinase-activated receptor 2 stimulation mediated by increase in intracellular cyclic AMP. J. Dermatol. Sci. 76(3), 206-213 (2014).