| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
PPNDS tetrasodium targets several proteins and receptors. It is a competitive inhibitor of meprin beta (IC50=80 nM, Ki=8 nM) and ADAM10 (IC50=1.2 microM). It is also a potent P2X1 receptor antagonist, showing up to 52-fold selectivity over P2Y1 receptors and no significant interaction with alpha1A-adrenoceptors or adenosine A1, A2B, histamine H1, and muscarinic M3 receptors. Furthermore, it functions as an agonist for the ATP receptor in Paramecium and inhibits viral RNA polymerases.
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| ln Vitro |
Meprin alpha (67 μM) and beta (IC50: 80 nM) are inhibited by PPNDS tetrasodium[1]. With an IC50 value of 0.88 μM, PPNDS tetrasodium (0-10 μM, 15 minutes) inhibits the murine norovirus RNA-dependent RNA polymerase (mNV-RdRp) [2]. Six viruses from the three calicivirus genera under test have their polymerases potently inhibited by PPNDS tetrasodium (0.025–10 µM; IC50 range: 0.1–2.3 µM) [4].
In vitro, PPNDS tetrasodium demonstrates potent and selective inhibition of its targets. It inhibits meprin beta with an IC50 of 80 nM and meprin alpha with an IC50 of 67 microM. It inhibits the murine norovirus RNA-dependent RNA polymerase (mNV-RdRp) with an IC50 of 0.88 microM. Furthermore, it potently inhibits polymerases from six viruses spanning the three Caliciviridae genera, with IC50 values ranging from 0.1 to 2.3 microM. |
| ln Vivo |
In vivo, PPNDS tetrasodium is primarily used for the study of meprin metalloproteases. In a mouse model of mesangial proliferative nephritis, a related compound (PPADS tetrasodium) was used to study mesangial cell proliferation in vivo, with intraperitoneal administration of 15-60 mg/100g body weight every 12 hours for 8 days. These studies help evaluate the potential therapeutic role of meprin beta inhibition in inflammatory diseases.
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| Enzyme Assay |
For non-cell-based enzyme inhibition assays, recombinant human meprin beta is incubated with varying concentrations of PPNDS tetrasodium (0-10,000 nM) and a fluorogenic substrate (e.g., Suc-Arg-Pro-Phe-AMC) in 50 mM Tris-HCl, 150 mM NaCl, and 10 microM ZnCl2 (pH 8.0) for 30-60 minutes at 37degC. Fluorescence (ex 340 nm, em 420 nm) is measured. IC50 is calculated from the dose-response curve. The Ki is determined using the Cheng-Prusoff equation.
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| Cell Assay |
For in vitro cell assays investigating antiviral activity, cells such as RAW 264.7 macrophages are seeded in multi-well plates and infected with murine norovirus (MNV). PPNDS tetrasodium is added at concentrations ranging from 0.025 to 10 uM for 15 minutes. After incubation, cells are lysed, and viral RNA is extracted. The reduction in viral RNA levels is quantified by RT-qPCR to assess the compound's inhibitory effect on viral replication.
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| Animal Protocol |
For in vivo studies of meprin inhibition, a mouse model of mesangial proliferative nephritis can be used. Mice receive PPNDS tetrasodium via intraperitoneal injection at a dose of 15-60 mg per 100g body weight, administered every 12 hours for 8 days. At the study endpoint, kidneys are harvested for histological analysis to evaluate mesangial cell proliferation. Blood samples are collected to measure markers of kidney function and inflammation.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for PPNDS tetrasodium is limited as it is a research reagent. The compound has a molecular weight of 694.36 g/mol and a molecular formula of C1₈H11N4Na4O14PS2. As a tetrasodium salt, it is highly water-soluble (e.g., 37.5 mg/mL in H2O). It is intended for in vitro and ex vivo use. Formulations for in vivo studies may use saline or other aqueous buffers. It is unstable in solution and should be prepared fresh.
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| Toxicity/Toxicokinetics |
As a research compound, PPNDS tetrasodium is not for human use. It is generally considered low-toxicity for in vitro applications at standard concentrations (micromolar range). A potential concern is the inhibition of meprin metalloproteases, which play roles in extracellular matrix remodeling. Specific acute or chronic toxicity data is not publicly available. Standard safety precautions (gloves, lab coat, goggles) should be used when handling the powder, which may be an irritant.
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| References | |
| Additional Infomation |
PPNDS tetrasodium is a multi-functional probe for studying several biological pathways simultaneously. It is a rare tool compound that acts as both a metalloprotease inhibitor (meprin beta/ADAM10) and a purinergic receptor antagonist (P2X1). It is valuable in inflammation research for dissecting the overlapping roles of meprin beta and ADAM10. Its ability to inhibit viral RNA polymerases also makes it a useful tool in virology for studying caliciviruses. It is not a clinical drug.
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| Molecular Formula |
C18H11N4NA4O14PS2
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| Molecular Weight |
694.361186265945
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| Exact Mass |
693.904
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| CAS # |
1021868-77-8
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| PubChem CID |
5311367
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| Appearance |
Brown to reddish brown solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
43
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| Complexity |
1170
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XHWIRFKQZFSILU-UHFFFAOYSA-J
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| InChi Code |
InChI=1S/C18H15N4O14PS2.4Na/c1-8-17(24)13(6-23)14(7-36-37(27,28)29)18(19-8)21-20-9-2-11-12(15(3-9)38(30,31)32)4-10(22(25)26)5-16(11)39(33,34)35;;;;/h2-6,24H,7H2,1H3,(H2,27,28,29)(H,30,31,32)(H,33,34,35);;;;/q;4*+1/p-4
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| Chemical Name |
tetrasodium;3-[[4-formyl-5-hydroxy-6-methyl-3-(phosphonatooxymethyl)pyridin-2-yl]diazenyl]-7-nitronaphthalene-1,5-disulfonate
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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) |
H2O : ~37.5 mg/mL (~54.01 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 | 1.4402 mL | 7.2009 mL | 14.4018 mL | |
| 5 mM | 0.2880 mL | 1.4402 mL | 2.8804 mL | |
| 10 mM | 0.1440 mL | 0.7201 mL | 1.4402 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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