A PDE4 inhibitor (IC50 = 2.2 nM for the human peripheral leukocyte enzyme); selective for PDE4 over PDE1

YM-976 – 5 mg

Brand:
Cayman
CAS:
191219-80-4
Storage:
-20
UN-No:
Non-Hazardous - /

YM-976 is a phosphodiesterase 4 (PDE4) inhibitor (IC50 = 2.2 nM for the human peripheral leukocyte enzyme).{46860} It is selective for PDE4 over PDE1, -2, -3, and -5 (IC50s = >3 µM for all). YM-976 inhibits LPS-induced TNF-α production in human peripheral blood mononuclear cells (PBMCs). In vivo, YM-976 inhibits carrageenan-induced pleural cavity cell infiltration in a rat model of pleurisy (ED30 = 9.1 mg/kg). It inhibits antigen-induced lung eosinophil infiltration in rats, mice, and ferrets (ED50s = 1.7, 5.8, and 1.2 mg/kg, respectively) and does not induce emesis in ferrets when administered at doses up to 10 mg/kg.{46861} YM-976 reduces ovalbumin-induced bronchoconstriction, as well as airway plasma leakage, eosinophil infiltration, and hyperreactivity in a guinea pig model of asthma (ED50s = 7.3, 5.7, 1, and 0.52 mg/kg, respectively).{46862} It also reduces citric acid-induced cough in guinea pigs.{46863}  

 

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Description

A PDE4 inhibitor (IC50 = 2.2 nM for the human peripheral leukocyte enzyme); selective for PDE4 over PDE1, -2, -3, and -5 (IC50s = >3 µM for all); inhibits LPS-induced TNF-α production in human PBMCs; inhibits carrageenan-induced pleural cavity cell infiltration in a rat model of pleurisy (ED30 = 9.1 mg/kg); inhibits antigen-induced lung eosinophil infiltration in rats, mice, and ferrets (ED50s = 1.7, 5.8, and 1.2 mg/kg, respectively); does not induce emesis in ferrets at doses up to 10 mg/kg; reduces ovalbumin-induced bronchoconstriction, as well as airway plasma leakage, eosinophil infiltration, and hyperreactivity in a guinea pig model of asthma (ED50s = 7.3, 5.7, 1, and 0.52 mg/kg, respectively); reduces citric acid-induced cough in guinea pigs

Formal name: 4-(3-chlorophenyl)-1,7-diethyl-pyrido[2,3-d]pyrimidin-2(1H)-one

Synonyms: 

Molecular weight: 313.8

CAS: 191219-80-4

Purity: ≥98%

Formulation: A solid

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