| Bioactivity | Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD)[1][2][3]. | ||||||||||||
| Invitro | Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions[2].Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response[2].Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood[2]. | ||||||||||||
| In Vivo | SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice[1].SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg[1].SB-207499 (500 μg/ear; b.i.d. for 6 d) inhibits the chronic oxazolone-induced inflammatory response and intralesional IL-4 concentrations in mice[1]. Animal Model: | ||||||||||||
| Name | Cilomilast | ||||||||||||
| CAS | 153259-65-5 | ||||||||||||
| Formula | C20H25NO4 | ||||||||||||
| Molar Mass | 343.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Griswold DE, et, al. SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11. [2]. Hatzelmann A, et, al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79. [3]. Barnette MS, et, al. SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions. J Pharmacol Exp Ther. 1998 Jan;284(1):420-6. |
Cilomilast
CAS: 153259-65-5 F: C20H25NO4 W: 343.42
Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~
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