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经验公式(希尔记法):
C9H6IN
化学文摘社编号:
分子量:
255.06
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
Ic1c2c(cncc2)ccc1
InChI key
CUILFTFMBBGSFT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
, yellow to light brown
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
DSRM-3716 is a potent and selective SARM1 NADase inhibitor (NAD+ hydrolysis IC50 = 75 nM using recombinant SARM1 SAM-TIR construct) that recapitulates the SARM1-/- phenotype and protects axons from degeneration induced by axotomy (EC50 = 2.1/1.9 µM by fragmentation/NfL release using mouse DRG neurons; 81/88% protection by 1/3 µM DSRM-3716 using human iPSC-derived motor neurons) or mitochondrial dysfunction (3-30 µM DSRM-3716 against 25 µM rotenone-induced injury; mouse DRG neurons). Mechanistically, DSRM-3716 undergoes base exchange with the nicotinamide (NAM) moiety of nicotinamide adenine dinucleotide (NAD+) to yield the bona fide inhibitor 1AD.
Potent and selective SARM1 NADase inhibitor that protects axons from degeneration induced by axotomy or mitochondrial dysfunction.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Dermal - Acute Tox. 4 Oral - Aquatic Chronic 3 - Eye Irrit. 2 - Skin Irrit. 2
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Structural basis of SARM1 activation, substrate recognition, and inhibition by small molecules.
Shi Y, et al.
Molecular Cell, 82, 1643-1659 (2022)
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