| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Ara-F-NAD⁺ sodium is a potent, reversible, slow-binding inhibitor of CD38 NADase, acting through competitive binding to the catalytic active site of the CD38 enzyme with an inhibition constant Ki of 169 nM . CD38 is a multifunctional ectoenzyme that primarily hydrolyzes NAD⁺ to ADP-ribose and nicotinamide.
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|---|---|
| ln Vitro |
In vitro studies demonstrate that Ara-F-NAD⁺ sodium effectively blocks NAD⁺ degradation by inhibiting CD38 NADase activity, thereby increasing intracellular NAD⁺ levels. This effect subsequently influences the activity of NAD⁺-dependent enzymes such as sirtuins and PARPs, which are involved in key cellular functions including DNA repair, mitochondrial biogenesis, and inflammation .
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| Enzyme Assay |
The inhibitory activity of this compound against CD38 is typically assessed using in vitro enzyme activity assays. A standard protocol involves pre-incubating purified recombinant CD38 enzyme with varying concentrations of Ara-F-NAD⁺ sodium in an appropriate reaction buffer, followed by the addition of the substrate NAD⁺ to initiate the reaction. The amount of reaction product (such as ADP-ribose) is detected by HPLC or fluorescence methods .
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| Cell Assay |
In cell-based studies, Ara-F-NAD⁺ sodium can be used to evaluate the effect of CD38 inhibition on NAD⁺ metabolism. The general protocol involves treating CD38-expressing cell lines with various concentrations of the compound for an appropriate duration, followed by measuring changes in intracellular NAD⁺ levels using NAD⁺/NADH assay kits or detecting CD38 enzyme activity changes via fluorescent probes .
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| Toxicity/Toxicokinetics |
Due to the arabino modification on the ribose moiety, this compound exhibits greater stability under physiological conditions compared to natural NAD⁺. The powder is stable for 3 years when stored at -20°C, and for 6 months at -80°C after dissolution .
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| References |
| Molecular Formula |
C21H25FN7NAO13P2
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|---|---|
| Molecular Weight |
687.40
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| Exact Mass |
687.0867303
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| Related CAS # |
Ara-F-NAD+;133575-27-6
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
45
|
| Complexity |
1120
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| Defined Atom Stereocenter Count |
8
|
| SMILES |
C1=CC(=C[N+](=C1)[C@H]2[C@@H]([C@@H]([C@H](O2)COP(=O)([O-])OP(=O)([O-])OC[C@@H]3[C@H]([C@H]([C@@H](O3)N4C=NC5=C(N=CN=C54)N)O)O)O)F)C(=O)N.[Na+]
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| InChi Key |
LOVZSFARRTXNIE-USDXJYMWSA-M
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| InChi Code |
InChI=1S/C21H26FN7O13P2.Na/c22-12-14(30)10(40-20(12)28-3-1-2-9(4-28)18(24)33)5-38-43(34,35)42-44(36,37)39-6-11-15(31)16(32)21(41-11)29-8-27-13-17(23)25-7-26-19(13)29;/h1-4,7-8,10-12,14-16,20-21,30-32H,5-6H2,(H5-,23,24,25,26,33,34,35,36,37);/q;+1/p-1/t10-,11-,12-,14-,15-,16-,20-,21-;/m1./s1
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| Chemical Name |
sodium [[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [(2R,3R,4R,5R)-5-(3-carbamoylpyridin-1-ium-1-yl)-4-fluoro-3-hydroxyoxolan-2-yl]methyl phosphate
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| Synonyms |
Ara-F-NAD+ (sodium); Ara-F-NAD+ sodium;
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4548 mL | 7.2738 mL | 14.5476 mL | |
| 5 mM | 0.2910 mL | 1.4548 mL | 2.9095 mL | |
| 10 mM | 0.1455 mL | 0.7274 mL | 1.4548 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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