| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
Xanthinol niacinate does not have a single specific target but acts as a vasodilator. It directly relaxes the smooth muscle of small arteries and capillaries, improving blood rheology and reducing peripheral vascular resistance. The niacinate (nicotinic acid) component may contribute to its vasodilatory effects through the release of prostaglandins. Xanthinol niacinate also displays anti-platelet and thrombolytic activity.
|
|---|---|
| ln Vitro |
In a dose-dependent manner, Xanthinol Nicotinate (Xanthinol Niacinate; 2.76-276 µM; for 24 hours) suppresses the proliferation of HUASMC [2]. PDGFR mRNA and PDGFR-β levels on the HUASMC cell membrane are dose-dependently decreased by xanthinol Nicotinate (2.76-276 µM; for 24 hours) [2].
Xanthinol niacinate acts as a vasodilator, directly relaxing the smooth muscle of small arteries and capillaries. It improves blood rheology and reduces peripheral vascular resistance. The compound also displays anti-platelet and thrombolytic activity. It has been shown to modulate tumors during their reoxygenation. |
| ln Vivo |
Tumor pO2 is quickly and momentarily altered by Xanthinol Nicotinate (75 mg/kg; IP); the highest pO2 levels are achieved 10 to 30 minutes after Xanthinol Nicotinate administration [1]. Niacin Xanthinol has the ability to radiosensitize tumors (radiation response enhanced by 1.4) when 10 Gy of X-rays are delivered during tumor reoxygenation [1].
Xanthinol niacinate has been shown to have a wide range of biological effects, including vasodilation and improved blood flow. It can modulate tumors during their reoxygenation and displays anti-platelet and thrombolytic activity. The compound is used in research to study its potential therapeutic effects in cardiovascular diseases and other conditions. |
| Enzyme Assay |
The in vitro assay for xanthinol niacinate typically involves measuring its vasodilatory effects on isolated blood vessels. Blood vessel segments are pre-contracted with a vasoconstrictor, and the compound is added at varying concentrations. The relaxation of the blood vessel is measured, and the EC50 is determined.
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Human Umbilical Artery Smooth Muscle Cells (HUASMC) Tested Concentrations: 2.76, 27.6 or 276 µM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of HUASMC proliferation in a dose-dependent manner. Western Blot Analysis[2] Cell Types: HUASMC Tested Concentrations: 2.76, 27.6 or 276 µM Incubation Duration: 24 hrs (hours) Experimental Results: PDGFR mRNA and PDGFR-β levels on the HUASMC cell membrane were dose-dependently diminished. The in vitro cellular assay for xanthinol niacinate typically involves culturing vascular smooth muscle cells. Cells are treated with varying concentrations of the compound, and cellular responses such as calcium mobilization or the production of vasodilatory mediators are measured. |
| Animal Protocol |
Animal/Disease Models: 5weeks old male NMRI mice [1]
Doses: 75 mg/kg Route of Administration: IP Experimental Results: Rapid and transient tumor pO2 changes and maximum pO2 values were obtained 10 to 30 minutes after XN administration. In vivo animal studies for xanthinol niacinate would typically involve the use of rodent models of cardiovascular disease. Animals would be administered the compound via oral or intravenous routes, and blood flow, blood pressure, and vascular resistance would be measured. The compound's effects on platelet aggregation and thrombus formation could also be assessed. |
| ADME/Pharmacokinetics |
Xanthinol niacinate has a molecular weight of 434.45 g/mol and a molecular formula of C19H26N6O6. The IUPAC name is 7-[2-hydroxy-3-[2-hydroxyethyl(methyl)amino]propyl]-1,3-dimethylpurine-2,6-dione;pyridine-3-carboxylic acid. The compound is soluble in DMSO (23 mg/mL, 52.94 mM). It is also known as xanthinol nicotinate.
|
| Toxicity/Toxicokinetics |
Xanthinol niacinate is generally well tolerated, but it is contraindicated in patients with myocardial infarction, mitral stenosis, and decompensated cardiac insufficiency, as well as in patients with acute hemorrhagic cerebrovascular disease and acute hemorrhagic disorders. The compound is intended for research use only.
|
| References |
[1]. Segers J, et al. Use of Xanthinol Nicotinate as a co-treatment for radio- and chemo-therapy in experimental tumors. Int J Cancer. 2010 Jan 15;126(2):583-8.
[2]. Bai X, et al. Inhibited proliferation of human umbilical artery smooth muscle cells by xanthinol nicotinate. Med Biol Eng Comput. 2016 Jun;54(6):891-8. |
| Additional Infomation |
A vasodilator used to treat peripheral vascular disease and dysfunction. It may cause stomach upset and low blood pressure.
Xanthinol niacinate (also known as xanthinol nicotinate) is a vasodilator that acts directly on the smooth muscle of small arteries and capillaries. It is a combination of xanthinol and niacin (nicotinic acid) and is used to improve blood flow and reduce peripheral vascular resistance. The compound is used in research to study its vasodilatory, anti-platelet, and thrombolytic effects. It has not yet entered clinical trials and is strictly for preclinical research purposes. |
| Molecular Formula |
C19H26N6O6
|
|---|---|
| Molecular Weight |
434.453
|
| Exact Mass |
434.191
|
| CAS # |
437-74-1
|
| PubChem CID |
9912
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
589.3ºC at 760 mmHg
|
| Melting Point |
180-184ºC
|
| Flash Point |
310.2ºC
|
| Vapour Pressure |
9.89E-15mmHg at 25°C
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
31
|
| Complexity |
548
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(CCO)CC(CN1C=NC2=C1C(=O)N(C)C(=O)N2C)O.C1=CC(=CN=C1)C(=O)O
|
| InChi Key |
GEPMAHVDJHFBJI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H21N5O4.C6H5NO2/c1-15(4-5-19)6-9(20)7-18-8-14-11-10(18)12(21)17(3)13(22)16(11)2;8-6(9)5-2-1-3-7-4-5/h8-9,19-20H,4-7H2,1-3H3;1-4H,(H,8,9)
|
| Chemical Name |
7-[2-hydroxy-3-[2-hydroxyethyl(methyl)amino]propyl]-1,3-dimethylpurine-2,6-dione;pyridine-3-carboxylic acid
|
| Synonyms |
NSC-113217; NSC 113217; Xanthinol niacinate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
H2O : ~250 mg/mL (~575.44 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (115.09 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3018 mL | 11.5088 mL | 23.0176 mL | |
| 5 mM | 0.4604 mL | 2.3018 mL | 4.6035 mL | |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3018 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
