A potent PDE4 inhibitor (IC50s = 4.9

GSK256066 – 5 mg

Brand:
Cayman
CAS:
801312-28-7
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}  

 

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SKU: 28012 - 5 mg Category:

Description

A potent PDE4 inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively); >380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and >2,500-fold selective over PDE7; inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM); intratracheal adminstration inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg); inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg)

Formal name: 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

Synonyms: 

Molecular weight: 518.6

CAS: 801312-28-7

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases

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