Dovramilast (CC-11050) 是一种磷酸二酯酶4(PDE4)抑制剂,具有口服活性,可以减少炎症反应,改善 INH 介导的肺部细菌清除。Dovramilast (CC-11050) 作为辅助试剂,用于结核病的研究。
产品描述
Dovramilast (CC-11050) is an oral phosphodiesterase 4 (PDE4) inhibitor and can reduce the inflammatory response and improves Isoniazid (INH)-mediated bacillary clearance from the lungs. Dovramilast (CC-11050), as an adjunct, is used for the research of tuberculosis (TB) [1].
体内活性
Dovramilast (oral gavage, 5, 25, or 50 mg/kg, single) significantly improves antibiotic-mediated bacterial killing and reduces lung pathology [2]. Pharmacokinetic Parameters of Dovramilast in B6D2F1 mice [2]. Sampling time(h) Concentration(ng/ml) CC-11050 only CC-11050+INH 1 1,331.6±136.97 905.35±594.23 2 1,409.47±140.85 1,309.39±214.08 5 948.85±128.7 1,609.18±167.2 8 820.6±265.98 1,271.73±249.18 24 1.27±1.1 4.96±1.85 T max (h) 2.0 5.0 C max (ng/ml) 1,410 1,610 AUC last (ng × h/ml) 10,200 13,900 Animal Model: B6D2F1 mice [2] Dosage: 5, 25, or 50 mg/kg Administration: oral, 5, 25, or 50 mg/kg, single Result: Reduced PDE4 expression in mtb-infected mouse lungs. Animal Model: B6D2F1 mice [2] Dosage: 5, 25, or 50 mg/kg Administration: oral gavage, 5, 25, or 50 mg/kg, single Result:
Cas No.
340019-69-4
分子式
C24H28N2O6S
分子量
472.55
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years