GSK-1482160 is a negative allosteric modulator of the P2X7 receptor (P2X7R), with high oral bioavailability and the ability to penetrate the blood-brain barrier. It has demonstrated a human pIC50 of 8.5 and a rat pIC50 of 6.5, effectively reducing ATP's efficacy at the receptor without altering its affinity, which subsequently inhibits IL-1β release. This compound serves as a valuable radioligand for P2X7R imaging using isotopes such as 11C or 18F and is applicable in research related to chronic joint pain and chronic constriction injury (CCI).
GSK-1482160 is a negative allosteric modulator of the P2X7 receptor (P2X7R), with high oral bioavailability and the ability to penetrate the blood-brain barrier. It has demonstrated a human pIC50 of 8.5 and a rat pIC50 of 6.5, effectively reducing ATP's efficacy at the receptor without altering its affinity, which subsequently inhibits IL-1β release. This compound serves as a valuable radioligand for P2X7R imaging using isotopes such as 11C or 18F and is applicable in research related to chronic joint pain and chronic constriction injury (CCI).
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