| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
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| Other Sizes |
| Targets |
IC50: 75 nM (SARM1 NADase)[1]
5-Iodoisoquinoline targets SARM1 (sterile alpha and TIR motif containing 1) NADase. SARM1 is a key regulator of axon degeneration, and its NADase activity is essential for this process. By inhibiting SARM1 NADase, 5-Iodoisoquinoline prevents the depletion of NAD+ and protects neurons from degeneration. |
|---|---|
| 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].
5-Iodoisoquinoline is a potent and selective SARM1 NADase inhibitor with an IC50 of 75 nM. It is selective against other NAD+-processing enzymes, receptors, and transporters. Its in vitro activity is assessed by measuring the inhibition of SARM1 NADase activity in enzyme assays. |
| ln Vivo |
5-Iodoisoquinoline has the potential to protect neurons from degeneration in vivo by inhibiting SARM1 NADase. Its in vivo efficacy can be assessed in animal models of axon degeneration, such as models of peripheral neuropathy or traumatic brain injury.
|
| Enzyme Assay |
The inhibition of SARM1 NADase by 5-Iodoisoquinoline can be assessed using an in vitro enzyme assay. SARM1 enzyme is incubated with its substrate, NAD+, in the presence of varying concentrations of the inhibitor. The production of ADP-ribose is measured, and the IC50 is determined.
|
| Cell Assay |
5-Iodoisoquinoline is used in cell-based assays to study its neuroprotective effects. Neurons are treated with the compound and then subjected to a stress that induces axon degeneration, such as axotomy or exposure to a neurotoxic agent. Axon degeneration is assessed by microscopy or by measuring axonal integrity.
|
| Animal Protocol |
5-Iodoisoquinoline is used in animal models of axon degeneration to study its neuroprotective effects. The compound is administered to animals, and the extent of axon degeneration is assessed by histological analysis or by measuring functional outcomes.
|
| ADME/Pharmacokinetics |
5-Iodoisoquinoline has a molecular weight of 255.06 g/mol and a molecular formula of C9H6IN. It is a solid that is soluble in DMSO. The compound is typically stored at -20°C.
|
| Toxicity/Toxicokinetics |
Toxicological data for 5-Iodoisoquinoline are not extensively detailed. It is not intended for human or veterinary use. Standard laboratory safety precautions, including the use of personal protective equipment (PPE), should be followed when handling the compound.
|
| References | |
| Additional Infomation |
5-Iodoisoquinoline (DSRM-3716) is a research-grade compound used as a potent and selective SARM1 NADase inhibitor. It is a valuable tool for studying the role of SARM1 in axon degeneration and for validating SARM1 as a therapeutic target for neurodegenerative diseases. The compound is not approved for therapeutic use and is strictly for laboratory research.
|
| 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
|
| SMILES |
C1=CC2=C(C=CN=C2)C(=C1)I
|
| 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)
|
| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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