DSRM-3716

Modify Date: 2024-01-06 19:41:55

DSRM-3716 Structure
DSRM-3716 structure
Common Name DSRM-3716
CAS Number 58142-99-7 Molecular Weight 255.06
Density 1.8±0.1 g/cm3 Boiling Point 336.8±15.0 °C at 760 mmHg
Molecular Formula C9H6IN Melting Point N/A
MSDS N/A Flash Point 157.5±20.4 °C

 Use of DSRM-3716


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[1].

 Names

Name 5-Iodoisoquinoline
Synonym More Synonyms

 DSRM-3716 Biological Activity

Description 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[1].
Related Catalog
Target

IC50: 75 nM (SARM1 NADase)[1]

In Vitro 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[1]. DSRM-3716 prevents neurofilament light chain (NfL) release from severed axons in a dose-dependent manner, with an IC50 of ~2 μM[1]. 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)[1]. DSRM-3716 inhibits the SARM1-dependent cell destruction pathway triggered by Rotenone in sensory neurons[1].
References

[1]. Robert O Hughes, et al. Small Molecule SARM1 Inhibitors Recapitulate the SARM1 -/- Phenotype and Allow Recovery of a Metastable Pool of Axons Fated to Degenerate. Cell Rep. 2021 Jan 5;34(1):108588.

 Chemical & Physical Properties

Density 1.8±0.1 g/cm3
Boiling Point 336.8±15.0 °C at 760 mmHg
Molecular Formula C9H6IN
Molecular Weight 255.06
Flash Point 157.5±20.4 °C
Exact Mass 254.954483
PSA 12.89000
LogP 2.99
Vapour Pressure 0.0±0.7 mmHg at 25°C
Index of Refraction 1.724
Storage condition 2-8°C

 Safety Information

Hazard Codes Xi

 Synthetic Route

~78%

DSRM-3716 Structure

DSRM-3716

CAS#:58142-99-7

Literature: Gamage, Swarna A.; Spicer, Julie A.; Rewcastle, Gordon W.; Milton, John; Sohal, Sukhjit; Dangerfield, Wendy; Mistry, Prakash; Vicker, Nigel; Charlton, Peter A.; Denny, William A. Journal of Medicinal Chemistry, 2002 , vol. 45, # 3 p. 740 - 743

~77%

DSRM-3716 Structure

DSRM-3716

CAS#:58142-99-7

Literature: Hamad Elgazwy, Abdel-Sattar S. Phosphorus, Sulfur and Silicon and Related Elements, 2000 , vol. 164, p. 131 - 143

~%

DSRM-3716 Structure

DSRM-3716

CAS#:58142-99-7

Literature: Hamad Elgazwy, Abdel-Sattar S. Phosphorus, Sulfur and Silicon and Related Elements, 2000 , vol. 164, p. 131 - 143

 Synonyms

5-Iodoisoquinoline
Isoquinoline, 5-iodo-
Isoquinoline,5-iodo
5-iodo-isoquinoline
5-Jod-isochinolin
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