A PDE4 inhibitor
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Cilomilast

Item No. 25979

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-cyclohexanecarboxylic acid
CAS Number
153259-65-5
Synonyms
  • SB 207499
Molecular Formula
C20H25NO4
Formula Weight
343.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 15mg/ml
λmax
232 nm
SMILES
COC1=C(OC2CCCC2)C=C([C@@]3(C#N)CC[C@H](C(O)=O)CC3)C=C1
InChi Code
InChI=1S/C20H25NO4/c1-24-17-7-6-15(12-18(17)25-16-4-2-3-5-16)20(13-21)10-8-14(9-11-20)19(22)23/h6-7,12,14,16H,2-5,8-11H2,1H3,(H,22,23)/t14-,20?
InChi Key
CFBUZOUXXHZCFB-FZOZEDLRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $145

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    10 mg

    $268

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    Product Description

    Cilomilast is a second generation inhibitor of phosphodiesterase 4 (PDE4; IC50 = 0.12 µM for the human enzyme).1,2 It is selective for human PDE4 over bovine PDE1, rat PDE2, and human PDE3 and -5 (IC50s = 74, 65, >100, and 83 µM, respectively).1 Cilomilast inhibits LPS-induced production of TNF-α in isolated human monocytes, as well as decreases production of leukotriene B4 (LTB4; Item No. 20110) induced by fMLP (Item No. 21495) in isolated human neutrophils (IC50s = 110 and 40 nM, respectively). It reduces ovalbumin-induced bronchoconstriction and pulmonary eosinophil infiltration in an ovalbumin-sensitized guinea pig model of asthma when administered at doses of 10 and 30 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Christensen, S.B., Guider, A., Forster, C.J., et al. 1,4-Cyclohexanecarboxylates: Potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma. Comparative Study 41(6), 821-835 (1998).

    2. Hatzelmann, A., and Schudt, C. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J. Pharmacol. Exp. Ther. 297(1), 267-279 (2001).