| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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Nudifloramide (2PY; 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxamide) is one of the end products from the degradation of nicotinamide-adenine dinucleotide (NAD). It inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro.
| ln Vitro |
Nicotinamide is not as effective as nudifloramide as a PARP-1 inhibitor [1].
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|---|---|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Uremic toxins often accumulate in the blood due to overeating or poor kidney filtration. Most uremic toxins are metabolic waste products that are normally excreted through urine or feces. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Uremic toxins, such as N-methyl-2-pyridone-5-carboxamide, can be actively transported to the kidneys via organic ion transporters, particularly OAT3. Elevated uremic toxin levels can stimulate the production of reactive oxygen species (ROS). This appears to be mediated by the direct binding of uremic toxins to or inhibition of NADPH oxidases, particularly NOX4, which is abundant in the kidneys and heart (A7868). ROS can induce a variety of different DNA methyltransferases (DNMTs) involved in the silencing of the KLOTHO protein. KLOTHO has been shown to play an important role in anti-aging, mineral metabolism, and vitamin D metabolism. Multiple studies have shown that in acute or chronic kidney disease, KLOTHO mRNA and protein levels are decreased due to elevated local ROS levels (A7869). |
| References | |
| Additional Infomation |
N-Methyl-6-pyridone-3-carboxamide is a pyridone with the structure 2-pyridone, where the C-5 position is substituted with a formamide group and the N-1 position is substituted with a methyl group. It is a metabolite, specifically a mouse metabolite. It is a pyridinecarboxamide, belonging to the pyridone class of compounds, and also a methylpyridine class of compounds. N1-Methyl-2-pyridone-5-carboxamide is a metabolite found in or produced by Escherichia coli (strains K12 and MG1655). 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxamide has been reported to exist in Mallotus macrostachyus, and relevant data exist. N-Methyl-2-pyridone-5-carboxamide is a uremic toxin. Based on their chemical and physical properties, uremic toxins can be classified into three main categories: 1) small, water-soluble, non-protein-bound compounds, such as urea; 2) small, lipid-soluble and/or protein-bound compounds, such as phenols; and 3) larger, so-called medium-molecule compounds, such as β2-microglobulins. Long-term exposure to uremic toxins can lead to various diseases, including kidney damage, chronic kidney disease, and cardiovascular disease. N-methyl-2-pyridone-5-carboxamide (2PY) is one of the end products of nicotinamide adenine dinucleotide (NAD) degradation. Elevated serum 2PY concentrations in patients with chronic renal failure (CRF), coupled with worsening renal function and its toxicity (significant inhibition of PARP-1), suggest that 2PY is an uremic toxin. (A3294)
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| Molecular Formula |
C7H8N2O2
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|---|---|
| Molecular Weight |
152.1506
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| Exact Mass |
152.058
|
| CAS # |
701-44-0
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| Related CAS # |
Nudifloramide-d3;1207384-48-2
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| PubChem CID |
69698
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
396.7±42.0 °C at 760 mmHg
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| Melting Point |
202-207ºC (dec.)
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| Flash Point |
193.7±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
-1.51
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
|
| Heavy Atom Count |
11
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| Complexity |
266
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JLQSXXWTCJPCBC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H8N2O2/c1-9-4-5(7(8)11)2-3-6(9)10/h2-4H,1H3,(H2,8,11)
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| Chemical Name |
1-methyl-6-oxopyridine-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 |
| 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) |
DMSO : ~62.5 mg/mL (~410.78 mM)
H2O : ~33.33 mg/mL (~219.06 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (13.67 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 20.8 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: ≥ 2.08 mg/mL (13.67 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 20.8 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: ≥ 2.08 mg/mL (13.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 20 mg/mL (131.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.5725 mL | 32.8623 mL | 65.7246 mL | |
| 5 mM | 1.3145 mL | 6.5725 mL | 13.1449 mL | |
| 10 mM | 0.6572 mL | 3.2862 mL | 6.5725 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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