| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
8-Br-NAD⁺ sodium is a prodrug that is converted intracellularly by the enzyme CD38 into its active metabolite, 8-bromo-cADPR (an inhibitor of cyclic ADP-ribose (cADPR)), thereby targeting and inhibiting cADPR-mediated calcium signaling pathways . Additionally, 8-Br-NAD⁺ itself can serve as a substrate in ADP-ribosylation reactions, acting on various NAD⁺-dependent enzymes .
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|---|---|
| ln Vitro |
In vitro studies demonstrate that 8-Br-NAD⁺ sodium (1 mM) prevents N-formyl-Met-Leu-Phe-induced increases in intracellular calcium levels and chemotaxis in isolated mouse bone marrow-derived neutrophils . At a concentration of 100 µM, this compound reduces LPS-induced nitrite production and decreases TNF-α and IL-2 secretion in mouse primary microglial cells .
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| Enzyme Assay |
As an NAD⁺ analog, 8-Br-NAD⁺ can be used as a substrate in ADP-ribosylation reactions in cell-free systems . A typical cell-free assay protocol involves incubating the purified target enzyme (such as CD38 or ART family proteins) with 8-Br-NAD⁺ in an appropriate reaction buffer (e.g., Tris-HCl containing Mg²⁺) to assess enzyme activity or substrate efficiency by detecting reaction products (such as 8-bromo-cADPR or ADP-ribosylated proteins).
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| Cell Assay |
For in vitro cellular assays, the activity of 8-Br-NAD⁺ sodium can be evaluated using neutrophil or microglial cell models. The specific protocol involves isolating mouse bone marrow-derived neutrophils or harvesting primary microglial cells, seeding them in culture plates, and pre-treating them with varying concentrations of 8-Br-NAD⁺ sodium (e.g., 1 mM or 100 µM). Following stimulation with agonists such as fMLP or LPS, intracellular calcium levels are detected using fluorescent probes (e.g., Fluo-4 AM), and TNF-α and IL-2 secretion in cell culture supernatants are measured by ELISA .
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| ADME/Pharmacokinetics |
As an NAD⁺ analog, the sodium salt form of this compound enhances its water solubility, and it exhibits good cell permeability . The compound should be stored at -80°C to maintain stability .
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| References |
| Molecular Formula |
C21H25BRN7NAO14P2
|
|---|---|
| Molecular Weight |
764.302996397018
|
| Exact Mass |
763.001
|
| CAS # |
2022926-16-3
|
| PubChem CID |
168445927
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
6
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
46
|
| Complexity |
1150
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C1=CC(=C[N+](=C1)C2C(C(C(O2)COP(=O)([O-])OP(=O)([O-])OCC3C(C(C(O3)N4C5=NC=NC(=C5N=C4Br)N)O)O)O)O)C(=O)N.[Na+]
|
| InChi Key |
OVUYJZJQRPYGFH-XKJOWHJHSA-M
|
| InChi Code |
InChI=1S/C21H26BrN7O14P2.Na/c22-21-27-11-16(23)25-7-26-18(11)29(21)20-15(33)13(31)10(42-20)6-40-45(37,38)43-44(35,36)39-5-9-12(30)14(32)19(41-9)28-3-1-2-8(4-28)17(24)34;/h1-4,7,9-10,12-15,19-20,30-33H,5-6H2,(H5-,23,24,25,26,34,35,36,37,38);/q;+1/p-1/t9-,10-,12-,13-,14-,15-,19-,20-;/m1./s1
|
| Chemical Name |
sodium;[[(2R,3S,4R,5R)-5-(6-amino-8-bromopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [(2R,3S,4R,5R)-5-(3-carbamoylpyridin-1-ium-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphate
|
| Synonyms |
8-bromo NAD+ (sodium salt); 8-Br-NAD+ sodium; 2022926-16-3; orb2276832
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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 |
| 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: ~50 mg/mL (65.4 mM)
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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 | 1.3084 mL | 6.5419 mL | 13.0839 mL | |
| 5 mM | 0.2617 mL | 1.3084 mL | 2.6168 mL | |
| 10 mM | 0.1308 mL | 0.6542 mL | 1.3084 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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