| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Sulfo-ara-F-NMN (CZ-48) targets two distinct enzymes: Sterile alpha and TIR motif containing 1 (SARM1) and CD38. It acts selectively, activating SARM1 while inhibiting CD38 with an IC50 around 10 microM. SARM1 is a key regulator of axonal degeneration and NAD+ depletion. CD38 is a cyclic ADP-ribose (cADPR) synthase and NAD+ hydrolase. By modulating these two enzymes, the compound influences cellular NAD+ levels and calcium signaling.
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| ln Vitro |
In the Toll-like receptor pathway, sterile alpha and Toll/interleukin-1 receptor motif-containing 1 (SARM1) is an adapter protein. SARM1 is activated by sulfo-ara-F-NMN, which results in the production of cyclic ADP-ribose and non-apoptotic cell death [1].
Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). It acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 microM). The compound induces the production of intracellular cyclic ADP-ribose (cADPR). This dual activity makes it a valuable tool for studying both SARM1-mediated axonal degeneration pathways and CD38-mediated NAD+ homeostasis and calcium mobilization. |
| ln Vivo |
Specific in vivo activity data for Sulfo-ara-F-NMN has not been published. As a SARM1 activator, it may be used to induce axonal degeneration in animal models of neurodegenerative diseases (e.g., Wallerian degeneration). As a CD38 inhibitor, it may elevate NAD+ levels, which could have beneficial effects in aging, metabolic disorders, and neurodegeneration. Its ability to induce intracellular cADPR may also affect calcium-dependent processes.
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| Enzyme Assay |
The specific protocol for evaluating SARM1 activation uses an in vitro NADase activity assay. Recombinant human SARM1 protein (TIR domain) is incubated with 100 uM NAD+ and varying concentrations of Sulfo-ara-F-NMN (1-100 uM) in assay buffer for 1 hour at 37degC. NAD+ consumption is quantified by adding an equal volume of 2% trichloroacetic acid to stop the reaction, followed by HPLC analysis of remaining NAD+. For CD38 inhibition, recombinant human CD38 is incubated with 50 uM etheno-NAD+ and varying concentrations of the compound, and the reaction product (etheno-cADPR) is measured by fluorescence.
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| Cell Assay |
For in vitro cellular assays, primary mouse dorsal root ganglion (DRG) neurons or SH-SY5Y neuroblastoma cells are used. Cells are treated with Sulfo-ara-F-NMN (CZ-48) at concentrations of 1-50 uM for 4-24 hours. NAD+ levels in cell lysates are measured using an NAD/NADH-Glo™ assay kit. cADPR levels are measured using a cyclic ADP-ribose ELISA kit. For SARM1 activation, axonal degeneration is assessed by imaging axonal morphology and quantifying neurite fragmentation. For CD38 inhibition, intracellular calcium flux (by Fluo-4 AM) can be measured following stimulation.
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| Animal Protocol |
An in vivo protocol for CZ-48 would involve a mouse model of Wallerian degeneration (sciatic nerve crush injury). Male C57BL/6 mice (8-10 weeks) undergo sciatic nerve crush injury under anesthesia. Sulfo-ara-F-NMN (CZ-48) is administered intraperitoneally at doses of 10-50 mg/kg daily for 7-14 days starting immediately after injury. Axonal degeneration is assessed by histological examination of sciatic nerve sections (toluidine blue staining) and by analysis of compound muscle action potentials (CMAP). Alternatively, for CD38 inhibition studies, the compound can be given to aged mice to assess NAD+ levels in liver and muscle tissues.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Sulfo-ara-F-NMN is not available. As a nucleotide analog (sulfated and fluorinated), it is likely to have poor oral bioavailability and a short half-life due to rapid metabolism by phosphatases and nucleotidases. For in vivo studies, it is typically administered intraperitoneally (IP) in aqueous buffers to achieve systemic exposure. The fluorine substitution may enhance metabolic stability compared to native NMN.
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| Toxicity/Toxicokinetics |
Toxicology data for Sulfo-ara-F-NMN is not available. As a compound that activates SARM1, which is a pro-degenerative protein, high doses could potentially induce axonal degeneration and neurotoxicity. Standard preclinical safety assessment would include acute toxicity studies in mice to determine the maximum tolerated dose (MTD) and a neurotoxicity assessment evaluating nerve function and histology. No significant toxicity has been reported at low micromolar concentrations.
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| References | |
| Additional Infomation |
Sulfo-ara-F-NMN (CZ-48) is a research-grade chemical and is not approved for clinical use. Its molecular formula is C11H14FN2O6PS with a molecular weight of 352.27. It is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 microM). It induces the production of intracellular cyclic ADP-ribose (cADPR). This compound is a valuable tool for studying NAD+ metabolism and the roles of SARM1 and CD38 in neurodegeneration, aging, and calcium signaling.
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| Molecular Formula |
C11H14FN2O6PS
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| Molecular Weight |
352.2758
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| Exact Mass |
352.029
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| CAS # |
1374663-29-2
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| PubChem CID |
146014460
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| Appearance |
White to light yellow solid powder
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| LogP |
-0.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
472
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S=P([O-])(O[H])OC([H])([H])[C@]1([H])[C@]([H])([C@@]([H])([C@]([H])([N+]2=C([H])C([H])=C([H])C(C(N([H])[H])=O)=C2[H])O1)F)O[H]
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| InChi Key |
SIQYQBAPGWSZQF-PKIKSRDPSA-N
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| InChi Code |
InChI=1S/C11H14FN2O6PS/c12-8-9(15)7(5-19-21(17,18)22)20-11(8)14-3-1-2-6(4-14)10(13)16/h1-4,7-9,11,15H,5H2,(H3-,13,16,17,18,22)/t7-,8+,9-,11-/m1/s1
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| Chemical Name |
1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-[[hydroxy(oxido)phosphinothioyl]oxymethyl]oxolan-2-yl]pyridin-1-ium-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ≥ 100 mg/mL (283.87 mM)
DMSO: 100 mg/mL (283.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.19 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 50.0 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: ≥ 5 mg/mL (14.19 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 50.0 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: ≥ 5 mg/mL (14.19 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 | 2.8387 mL | 14.1933 mL | 28.3865 mL | |
| 5 mM | 0.5677 mL | 2.8387 mL | 5.6773 mL | |
| 10 mM | 0.2839 mL | 1.4193 mL | 2.8387 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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