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 |
供货周期: | 一周 |
品牌: | |
规格: | 2mg |
货号: | K1367 |
CAS号: | 801312-28-7 |
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 |
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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