Catalog No.S7937 Synonyms: Nemiralisib
Molecular Weight(MW): 440.54
Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).
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|Description||Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor(pKi = 9.9).|
|In vivo||GSK-2269557 has low oral bioavailability (F=2%) and in vivo clearance of 28 mL/min/kg but has a high volume of distribution of 6.3 L/kg. GSK-2269557 induces concentration-dependent increases in QT interval and Tp-e at 0.3 and 1 μM (1 and 0.5 Hz) and an increase in QRS at 1 μM (2 Hz), however, no treatment-related torsades de pointes (TdP) arrhythmias are observed. In a disease relevant brown Norway rat acute OVA model of Th2 driven lung inflammation, GSK-2269557 is shown to protect against eosinophil recruitment with an ED50 of 67 μg/kg and dose-dependently reduces recruitment of all leukocyte subpopulations and IL-13 in the lungs.|
|In vitro||DMSO||88 mg/mL (199.75 mM)|
|Ethanol||8 mg/mL (18.15 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01762878||Completed||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||January 9 2013||Phase 1|
|NCT02522299||Completed||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||November 4 2015||Phase 2|
|NCT02294734||Completed||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||March 31 2015||Phase 2|
|NCT02130635||Completed||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||July 31 2014||Phase 2|
|NCT03345407||Active not recruiting||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||November 28 2017||Phase 2|
|NCT01462617||Completed||Asthma||GlaxoSmithKline||July 24 2011||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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