A PDE4 inhibitor (IC50 = 0.31 nM); selective for PDE4 over PDE1

Piclamilast – 10 mg

Brand:
Cayman
CAS:
144035-83-6
Storage:
-20
UN-No:
Non-Hazardous - /

Piclamilast is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 0.31 nM).{52090} It is selective for PDE4 over PDE1, PDE2, PDE3, PDE5, and PDE7A in cell-free assays (IC50s = >100, 40, >100, 14, and >10 μM, respectively).{52091,52089} Piclamilast inhibits superoxide production by guinea pig eosinophils and histamine-induced contraction in isolated guinea pig trachea (IC50s = 24 and 2 nM, respectively).{52090,52088} It inhibits eosinophil, neutrophil, lymphocyte, and TNF-α accumulation in bronchoalveolar lavage fluid (BALF) from ovalbumin-sensitized rats (ED50s = 23.8, 14.1, 19.5, and 14.4 μmol/kg, respectively).{52087} Piclamilast also inhibits ovalbumin-induced bronchoconstriction in a guinea pig model of asthma (ED50 = 0.033 mg/kg).{52091}  

 

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Description

A PDE4 inhibitor (IC50 = 0.31 nM); selective for PDE4 over PDE1, PDE2, PDE3, PDE5, and PDE7A in cell-free assays (IC50s = >100, 40, >100, 14, and >10 μM, respectively); inhibits superoxide production by guinea pig eosinophils and histamine-induced contraction in isolated guinea pig trachea (IC50s = 24 and 2 nM, respectively); inhibits eosinophil, neutrophil, lymphocyte, and TNF-α accumulation in bronchoalveolar lavage fluid (BALF) from ovalbumin-sensitized rats (ED50s = 23.8, 14.1, 19.5, and 14.4 μmol/kg, respectively); nhibits eosinophil, neutrophil, lymphocyte, and TNF-α accumulation in BALF from ovalbumin-sensitized rats (ED50s = 23.8, 14.1, 19.5, and 14.4 μmol/kg, respectively); inhibits ovalbumin-induced bronchoconstriction in a guinea pig model of asthma (ED50 = 0.033 mg/kg)

Formal name: 3-(cyclopentyloxy)-N-(3,5-dichloro-4-pyridinyl)-4-methoxy-benzamide

Synonyms:  RP 73401|RPR 73401

Molecular weight: 381.3

CAS: 144035-83-6

Purity: ≥98%

Formulation: A solid

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