A PDE4 inhibitor (IC50 = 0.12 µM for the human enzyme); selective for human PDE4 over bovine PDE1

Cilomilast – 1 mg

Brand:
Cayman
CAS:
153259-65-5
Storage:
-20
UN-No:
Non-Hazardous - /

Cilomilast is a second generation inhibitor of phosphodiesterase 4 (PDE4; IC50 = 0.12 µM for the human enzyme).{49691,49692} It is selective for human PDE4 over bovine PDE1, rat PDE2, and human PDE3 and -5 (IC50s = 74, 65, >100, and 83 µM, respectively).{49691} Cilomilast inhibits LPS-induced production of TNF-α in isolated human monocytes, as well as decreases production of leukotriene B4 (LTB4; Item No. 20110) induced by fMLP (Item No. 21495) in isolated human neutrophils (IC50s = 110 and 40 nM, respectively). It reduces ovalbumin-induced bronchoconstriction and pulmonary eosinophil infiltration in an ovalbumin-sensitized guinea pig model of asthma when administered at doses of 10 and 30 mg/kg.{49691}  

 

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SKU: 25979 - 1 mg Category:

Description

A PDE4 inhibitor (IC50 = 0.12 µM for the human enzyme); selective for human PDE4 over bovine PDE1, rat PDE2, and human PDE3 and -5 (IC50s = 74, 65, >100, and 83 µM, respectively); inhibits LPS-induced production of TNF-α in isolated human monocytes, as well as decreases fMLP-induced LTB4 production in isolated human neutrophils (IC50s = 110 and 40 nM, respectively); reduces ovalbumin-induced bronchoconstriction and pulmonary eosinophil infiltration in an ovalbumin-sensitized guinea pig model of asthma at 10 and 30 mg/kg

Formal name: cis-4-cyano-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-cyclohexanecarboxylic acid

Synonyms:  SB 207499

Molecular weight: 343.4

CAS: 153259-65-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Immunology & Inflammation|Pulmonary Diseases|COPD/Emphysema

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