6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
GSK256066
CAS: 801312-28-7
Molecular Formula: C27H26N4O5S
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide - Names and Identifiers
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide - Physico-chemical Properties
| Molecular Formula | C27H26N4O5S |
| Molar Mass | 518.58 |
| Density | 1.345 |
| Boling Point | 791.7±60.0 °C(Predicted) |
| pKa | 15.01±0.30(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | GSK256066 is a slow but tightly bound PDE4B inhibitor with an IC50 of 3.2 pM. GSK256066 acts on PBMCs and potently inhibits LPS-stimulated TNFα production with pIC50 of 11.0 and IC50 of 10 pM, and GSK256066 acts on human whole blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 inhibits PDE4 with high selectivity (3.8 × 105 times more than that of PDE1,PDE2, PDE3, PDE5, and PDE6, and 2.5 × 103 times more than that of PDE7). GSK256066 inhibited PDE4 subtype A- D with equivalent affinity. GSK256066 is a slow but tightly bound PDE4B inhibitor with an IC50 of 3.2 pM. GSK256066 acts on PBMCs and potently inhibits LPS-stimulated TNFα production with pIC50 of 11.0 and IC50 of 10 pM, and GSK256066 acts on human whole blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 highly selective inhibition of PDE4 (3.8 × 10 that inhibits PDE1,PDE2, PDE3, PDE5, and PDE6) |
| In vivo study | GSK256066 was administered in aqueous suspension to inhibit LPS-induced pulmonary neutrophils with an ED50 of 1.1 μg/kg, with a maximum inhibition of 72% at a dose of 30 μg/kg. GSK256066 was administered as a dry powder preparation to inhibit LPS-induced pulmonary neutrophils, and the ED50 was 2.9 μg/kg, which was the maximum inhibition of 62%. GSK256066 acts on male CD rats, with a mild plasma clearance rate of 39 ml/min/kg, a moderate volume of distribution, 0.8 L/kg, and a relatively short half-life, 1.1 hours. GSK256066 was administered intratracheally at a dose of 30 μg/kg in aqueous suspension to maintain a high lung concentration of 2.6 μg/g. GSK256066 at a dose of 10 μg/kg at different times (2, 6, 12, 18, 24, and 36 h) intratracheal treatment, and then LPS treatment, then inhibit lipopolysaccharide (LPS) LPS-induced pulmonary neutrophilia in the induced acute Pneumonia rat model. GSK256066 at doses of 0.3-100 μg/kg inhibited the LPS-induced increase in exhaled NO with an ED50 of 35 μg/kg. Treatment of rats with GSK256066 at a dose of 10 μg/kg for half an hour followed by OVA inhibited OVA-induced lung eosinophilia with an ED50 of 0.4 μg/kg. GSK256066 was administered in aqueous suspension to inhibit LPS-induced pulmonary neutrophils with an ED50 of 1.1 μg/kg and a dose of 30 μg/kg, then the maximum inhibition was 72%. GSK256066 was administered as a dry powder preparation to inhibit LPS-induced pulmonary neutrophils, and the ED50 was 2.9 μg/kg, which was the maximum inhibition of 62%. GSK256066 acts on male CD rats, with a mild plasma clearance rate of 39 ml/min/kg, a moderate volume of distribution, 0.8 L/kg, and a relatively short half-life, 1.1 hours. GSK256066 was administered intratracheally at a dose of 30 μg/kg in aqueous suspension to maintain a high lung concentration of 2.6 μg/g. GSK256066 at a dose of 10 μg/kg at different times (2, 6, 12, 18, 24, and 36 h) intratracheal treatment followed by LPS inhibited LPS-induced pulmonary neutrophilia in the lipopolysaccharide (LPS)-induced acute Pneumonia rat model. GSK256066 at doses of 0.3-100 μg/kg inhibited the LPS-induced increase in exhaled NO with an ED50 of 35 μg/kg. Treatment of rats with GSK256066 at a dose of 10 μg/kg for half an hour followed by OVA inhibited OVA-induced lung eosinophilia with an ED50 of 0.4 μg/kg. |
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.928 ml | 9.642 ml | 19.283 ml |
| 5 mM | 0.386 ml | 1.928 ml | 3.857 ml |
| 10 mM | 0.193 ml | 0.964 ml | 1.928 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.386 ml |
Last Update：2024-01-02 23:10:35
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Product Name: GSK256066 Visit Supplier Webpage Request for quotation
CAS: 801312-28-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 801312-28-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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