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    Cilomilast
    Cilomilast

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0779
    CAS #: 153259-65-5Purity ≥98%

    Description: Cilomilast (also known as Ariflo and SB-207,499) is a novel, potent and orally bioactive PDE4 inhibitor with IC50 of about 110 nM, it has anti-inflammatory activity and low central nervous system activity. 

    References: J Pharmacol Exp Ther. 1998 Nov;287(2):705-11; Int Immunopharmacol. 2011 Jun;11(6):732-9.

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    Molecular Weight (MW)343.42
    FormulaC20H25NO4
    CAS No.153259-65-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (200.9 mM)
    Water: <1 mg/mL
    Ethanol: 50 mg/mL (145.6 mM)
    Solubility (In vivo)5% DMSO+95% Corn oil: 30 mg/mL
    SynonymsCilomilast; SB 207499; SB207499; Ariflo; SB-207499; 

    Chemical Name: cis-4-Cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]cyclohexanecarboxylic acid

    InChi Key: CFBUZOUXXHZCFB-LDTOLXSISA-N

    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+

    SMILES Code: O=C([[email protected]]1CC[[email protected]](C2=CC=C(OC)C(OC3CCCC3)=C2)(C#N)CC1)O           


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    In Vitro

    In vitro activity: Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. Cilomilast produces a concentration-dependent increase in cAMP content in U937 cells. In isolated human monocytes, Cilomilast and (R)-rolipram are equipotent at suppressing LPS-induced TNF-α formation with -log (IC50) of 7.0 and 7.2, respectively. Both Cilomilast and (R)-rolipram produces a modest prevention of fMLP-induced degranulation of human neutrophils. Cilomilast and (R)-rolipram are equipotent at suppressing neutrophil activation with -log (IC50) of 7.1 and 6.4, respectively. Cilomilast significantly decreases the expression of TNF-α in the cornea and IL-1α, IL-1β, and TNF-α in the conjunctivaas compared to vehicle control. Cilomilast treatment markedly decreases the presence of CD11b+ antigen-presenting cells in the central and peripheral cornea, and leads to decreased conjunctival expression of cytokines IL-6, IL-23, and IL-17. Moreover, Cilomilast decreases the expression of IL-17 and IL-23 in the draining lymph nodes. Cilomilast reduces TLR4 expression, IL-8 release and neutrophil chemotactic activity as well as it increased IP-10 release and lymphocyte chemotactic activity.


    Kinase Assay: Cilomilast(SB 207499; Ariflo) is a potent PDE4 inhibitor with IC50 of about 110 nM, has anti-inflammatory activity and low central nervous system activity. IC50 value: 110 nM Target: PDE 4 Cilomilast (SB-207499) inhibits HPDE4 and LPDE4 catalytic activity with equal potency (Ki ≈100 nM). SB-207499 and rolipram are equipotent against LPDE4, but Cilomilast (Ariflo, SB-207499) is 100-fold less potent against HPDE4. This profile suggests that Cilomilast (Ariflo, SB-207499) retain the anti-inflammatory activity of rolipram yet have a decreased tendency to produce side effects.


    Cell Assay: U937 cells (1-2 × 10 6) are incubated at 37 °C in a shaking water bath with Cilomilast for 1 min before the addition of 0.1 μM PGE2 (total volume of 200 μL). The incubation proceeds for an additional 4 min and is stopped by the addition of 0.1 mL of HClO4 (17.5%), neutralized with 0.15 ml of K23 (1.0 M) and diluted to 1 mL with sodium acetate buffer. Samples are centrifuged at 3000 × g for 10 min. Aliquots of the supernatant fraction are assayed for cAMP content by radioimmunoassay using commercially available kits.

    In VivoCilomilast inhibits human TNFα production with oral ED50 of 4.9 mg/kg. In contrast to their equipotent activity against TNFα production, Cilomilast (ED50 = 2.3 mg/kg, p.o.) is 10-fold less potent than R-rolipram (ED50 = 0.23 mg/kg, p.o.) in reversing reserpine-induced hypothermia, a model of antidepressant activity. In time course studies, Cilomilast (30 mg/kg, p.o.) suppresses TNFα production for at least 10 hour. The ability of Cilomilast to modulate interleukin-4 productionin vivo is assessed in a chronic oxazolone-induced contact sensitivity model in Balb/c mice. Topical administration of Cilomilast (1000 μg) inhibits intralesional concentrations of interleukin-4. Orally administered cilomilast dose-dependently inhibits production of interleukin-4, TNF-α, and cysteinyl leukotrienes, as well as leukocyte infiltration in bronchoalveolar lavage fluid from the airways of ovalbumin-sensitized Brown Norway rats.
    Animal modelBalb/c, CD-1 and C57B1/6 male mice weighing from 18 to 25 g with human monocytes or endotoxin-induced shock
    Formulation & DosageDissovled in Olive oil; 3, 6, 12, 25, 50 mg/kg; oral gavage
    ReferencesJ Pharmacol Exp Ther. 1998 Nov;287(2):705-11; Int Immunopharmacol. 2011 Jun;11(6):732-9.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Cilomilast

    Inhibition of human TNFα by orally administered SB 207499 (Cilomilast) (A) or R-rolipram (B). J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.
     

    Cilomilast

    Reversal of reserpine-induced hypothermia by R-rolipram (○) or SB 207499 (•). J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.
     

    Cilomilast

    Pharmacokinetic/pharmacodynamic relationship for SB 207499. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.


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