YL-365 is a potent and selective antagonist of the GPR34 receptor, exhibiting an IC50 value of 17 nM. By binding to a specific region within the orthosteric binding pocket, YL-365 induces allosteric modifications that stabilize the receptor in an inactive state. It effectively down-regulates the pro-inflammatory gene iNOS in M1 microglia, consequently suppressing pro-inflammatory responses. Additionally, YL-365 demonstrates dose-dependent reduction of mechanical allodynia in mouse models of neuropathic pain, making it a valuable tool for studying inflammatory mechanisms and potential treatments for neuropathic conditions.
YL-365 is a potent and selective antagonist of the GPR34 receptor, exhibiting an IC50 value of 17 nM. By binding to a specific region within the orthosteric binding pocket, YL-365 induces allosteric modifications that stabilize the receptor in an inactive state. It effectively down-regulates the pro-inflammatory gene iNOS in M1 microglia, consequently suppressing pro-inflammatory responses. Additionally, YL-365 demonstrates dose-dependent reduction of mechanical allodynia in mouse models of neuropathic pain, making it a valuable tool for studying inflammatory mechanisms and potential treatments for neuropathic conditions.
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