GSK256066

GSK256066

参考价:¥2057
供货周期: 一周
品牌:
规格: 2mg
货号: K1367
CAS号: 801312-28-7
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SKU:K1367   M. Wt:518.58  
Formula:C27H26N4O5S   Solubility:No  
Purity:>99%   Storage:2 years at -20 degrees centigrade  
CAS No.:801312-28-7   Synonyms:N/A  
Chemical NameN/A
Biological Activity
Description GSK256066
Targets PDE4B        
IC50 3.2 pM        
In vitro GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFalpha production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM.
In vivo GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 ug/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat.
Clinical Trials N/A
Features N/A

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