Cilomilast

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 PDE4 抑制剂，对 LPDE4/HPDE4 的 IC50 为 95/120 nM。

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.

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.

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.

SB-207499 | SB207499 | SB 207499

Angiogenesis

PDE

HPDE4|LPDE4

Inflammation/Immunology

COPD

153259-65-5

343.4168

C20H25NO4

>98% (HPLC)

10 mM in DMSO

O=C([C@H]1CC[C@](C2=CC=C(OC)C(OC3CCCC3)=C2)(C#N)CC1)O

Cyclohexanecarboxylic acid, 4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-, cis-

(-20℃)

With Ice Pack

≥ 2 years