DSRM-3716 (5-Iodoisoquinoline) is a potent and specific SARM1 NADase inhibitor (antagonist) with IC50 of 75 nM. DSRM-3716 is selective for other NAD+ processing enzymes, receptors and transporters. DSRM-3716 has potent axonal protection.

Physicochemical Properties

Molecular Formula	C9H6IN
Molecular Weight	255.06
Exact Mass	254.954
CAS #	58142-99-7
PubChem CID	11391181
Appearance	Yellow to brown solid powder
Density	1.8±0.1 g/cm3
Boiling Point	336.8±15.0 °C at 760 mmHg
Flash Point	157.5±20.4 °C
Vapour Pressure	0.0±0.7 mmHg at 25°C
Index of Refraction	1.724
LogP	2.99
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	1
Rotatable Bond Count	0
Heavy Atom Count	11
Complexity	138
Defined Atom Stereocenter Count	0
InChi Key	CUILFTFMBBGSFT-UHFFFAOYSA-N
InChi Code	InChI=1S/C9H6IN/c10-9-3-1-2-7-6-11-5-4-8(7)9/h1-6H
Chemical Name	5-iodoisoquinoline
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	IC50: 75 nM (SARM1 NADase)[1]
ln Vitro	In these cultures, treatment with DSRM-3716 results in dose-dependent suppression of the increase in cADPR (IC50 of 2.8 μM) and significant preservation of NAD+. This is in line with the engagement and suppression of SARM1 enzymatic NADase activity within the cells[1]. ?Neurofilament light chain (NfL) release from severed axons is inhibited by DSRM-3716 in a dose-dependent manner, with an IC50 of approximately 2 μM[1]. DSRM-3716 has the same potency (IC50 of 2.8 μM) to prevent axonal degeneration as it does to inhibit the increase in cADPR brought on by axotomy[1]. The SARM1-dependent cell destruction pathway in sensory neurons that is triggered by rotenone is inhibited by DSRM-3716[1].
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO: 50 mg/mL (196.03 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (9.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (9.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.9206 mL	19.6032 mL	39.2065 mL
	5 mM	0.7841 mL	3.9206 mL	7.8413 mL
	10 mM	0.3921 mL	1.9603 mL	3.9206 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.