DSRM-3716 (5-Iodoisoquinoline) is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. DSRM-3716 is selective against other NAD-processing enzymes, receptors, and transporters. DSRM-3716 provides robust axon protection.
体外研究
DSRM-3716 treatment produces dose-dependent inhibition of cADPR increase (IC50 of 2.8 μM) and substantial preservation of NAD in these cultures in a manner consistent with engagement and inhibition of SARM1 enzymatic NADase activity inside the cells.
DSRM-3716 prevents neurofilament light chain (NfL) release from severed axons in a dose-dependent manner, with an IC50 of ~2 μM.
The potency of DSRM-3716 to inhibit cADPR increase caused by axotomy (IC50 of 2.8 μM) is similar to the potency required to prevent axonal degeneration (IC50 of 2.1 μM).
DSRM-3716 inhibits the SARM1-dependent cell destruction pathway triggered by Rotenone in sensory neurons.
分子式
C9H6In
分子量
255.06
CAS号
58142-99-7
中文名称
5-碘异喹啉
运输条件
Room temperature in continental US; may vary elsewhere.