A selective inhibitor of PDE4 (IC50 = 1.27 μM for PDE4 versus >100 μM for PDE1

CP 80,633 – 10 mg

Brand:
Cayman
CAS:
135637-46-6
Storage:
-20
UN-No:
Non-Hazardous - /

Phosphodiesterases (PDE) enzymatically convert the cyclic nucleotide second messengers cAMP and cGMP to 5’-AMP and 5’-GMP, respectively, thus terminating signal transduction. The cAMP-specific PDE4 isoforms may be particularly important in certain respiratory and neurological diseases. CP 80,633 is a selective inhibitor of PDE4 (IC50 = 1.27 μM for PDE4 versus. >100 μM for PDE1, PDE2, PDE3, and PDE5).{18129} It potentiates PGE1-dependent increases in cAMP levels in eosinophils, monocytes, and T-cells, inhibits eosinophil superoxide production (IC50 induced TNF-α release from monocytes (IC50 = 0.22 μM).{18129} CP 80,633 (1 mg/kg) significantly reduces antigen-induced airway inflammation in atopic guinea pigs, monkeys, and mice.{18130,18131}  

 

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Description

A selective inhibitor of PDE4 (IC50 = 1.27 μM for PDE4 versus >100 μM for PDE1, PDE2, PDE3, and PDE5); inhibits eosinophil superoxide production (IC50 induced TNFα release from monocytes ,(IC50 = 0.22 μM); significantly reduces antigen-induced airway inflammation in atopic guinea pigs, monkeys, and mice

Formal name: 5-[3-[(1S,2S,4R)-bicyclo[2.2.1]hept-2-yloxy]-methoxyphenyl]tetrahydro-2-(1H)-pyrimidinone

Synonyms: 

Molecular weight: 316.4

CAS: 135637-46-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

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