Cilomilast

SKU: orb1226139

Description

A potent and selective PDE4 inhibitor with IC50 of 95/120 nM for LPDE4/HPDE4; shows selectivity for PDE4 over the other PDE isozymes and is 75-fold more selective than (R)-rolipram with respect to LPDE4 activity versus HPDE4 activity; inhibits antigen-induced bronchoconstriction in conscious guinea pigs at 30 mg/kg and orally acitive.COPD Phase 3 Discontinued(In Vitro):Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions.Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response.Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood.(In Vivo):SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice.SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg.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.

Key Properties

• CAS Number: 153259-65-5
• MW: 343.4168
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₅NO₄
• SMILES: O=C([C@H]1CC[C@](C2=CC=C(OC)C(OC3CCCC3)=C2)(C#N)CC1)O
• Target: PDE
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  SB-207499 (1-100 mg/kg; p.o.) significantly inhibits the production of human TNFα in a dose-dependent manner in mice. SB-207499 (0.1-100 mg/kg; oral gavage) reverses reserpine-induced hypothermia in mice, with an ED50 of 2.3 mg/kg. 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. Animal model: Male Balb/c mice (18-25 g) are injected with human monocytes and LPS. Dosage: 1, 5, 10, 50, 100 mg/kg. Administration: p.o. after the injection of human monocytes and before LPS challenge. Result: Inhibited the production of human TNFα, with an ED50 of 4.9 mg/kg.
• In Vitro:
  Cilomilast (0.1 nM-10 μM; 5 min) inhibits human neutrophil functions. Cilomilast (0.1 nM-10 μM; 5 min) inhibits eosinophil chemiluminescence response. Cilomilast (0.001-100 μM; 30 min) inhibits the synthesis of TNFα in human monocytes and in human whole blood.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB-207499 | SB207499 | SB 207499

Quick Database Links

Gene Symbol

PDE