Names
| Name | 1-[5-tert-butyl-2-(3-chloro-4-hydroxyphenyl)pyrazol-3-yl]-3-[[2-[[3-[2-(2-hydroxyethylsulfanyl)phenyl]-[1,2,4]triazolo[4,3-a]pyridin-6-yl]sulfanyl]phenyl]methyl]urea |
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| Synonym | More Synonyms |
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PF-03715455 Biological Activity
| Description | PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease)[1][2]. |
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| Related Catalog | Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK Research Areas >> Inflammation/Immunology |
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| Target | p38α:0.88 nM (IC50) p38β:23 nM (IC50) |
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| In Vitro | PF-03715455 is a moderate inhibitor of CYP1A2, CYP2C19, and CYP2D6 and a potent inhibitor of CYP’s 2C9 and CYP3A4[2]. |
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| In Vivo | PF-03715455 treatment shows that the Vss and T1/2 are 0.19 L/kg, 1 hour, respectively[2]. Animal Model: Male CD Sprague Dawley rats (300-450 g)[2] Dosage: 1 mg/kg Administration: I.v. (Pharmacokinetic Analysis) Result: The Vss, and T1/2 were 0.19 L/kg, 1 hour, respectively. |
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| References | [1]. Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. [2]. Millan DS, et al. Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. J Med Chem. 2011 Nov 24;54(22):7797-814. |
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Chemical & Physical Properties
| Molecular Formula | C35H34ClN7O3S2 |
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| Molecular Weight | 700.27300 |
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| Exact Mass | 699.18500 |
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| PSA | 183.69000 |
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| LogP | 8.07320 |
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Company Profile
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