Xanthinol Nicotinate
(Synonyms: 烟酸占替诺; Xanthinol Niacinate) 目录号 : GC39674
Xanthinol Nicotinate (Complamin, Angioamin) is a potent vasodilator that can easily pass through the cell membrane and once inside the cell it causes an increase in glucose metabolism resulting in an increased energy.
Cas No.:437-74-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Xanthinol Nicotinate (Complamin, Angioamin) is a potent vasodilator that can easily pass through the cell membrane and once inside the cell it causes an increase in glucose metabolism resulting in an increased energy.
| Cas No. | 437-74-1 | SDF | |
| 别名 | 烟酸占替诺; Xanthinol Niacinate | ||
| Canonical SMILES | O=C(C1=CC=CN=C1)O.O=C(N2C)N(C)C3=C(N(CC(O)CN(CCO)C)C=N3)C2=O | ||
| 分子式 | C19H26N6O6 | 分子量 | 434.45 |
| 溶解度 | Water: 250 mg/mL (575.44 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Chemoenzymatic synthesis of enantiomerically enriched diprophylline and Xanthinol Nicotinate
Bioorg Chem 2021 Jan;106:104448.PMID:33229120DOI:10.1016/j.bioorg.2020.104448.
A concise chemoenzymatic route toward enantiomerically enriched active pharmaceutical ingredients (API) - diprophylline and Xanthinol Nicotinate - is reported for the first time. The decisive step is an enantioselective lipase-mediated methanolysis of racemic chlorohydrin-synthon acetate, namely 1-chloro-3-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)propan-2-yl acetate, performed under kinetically-controlled conditions on a preparative 500 mg-scale. The best results in terms of reaction enantioselectivity (E = 14) were obtained for the enantiomers resolution performed with lipase type B from Candida antarctica immobilized on acrylic resin (CAL-B, Novozym 435) suspended in homophasic acetonitrile-methanol mixture. The elaborated biocatalytic system furnished the key chlorohydrin intermediate (in 71% ee and 38% yield), which was then smoothly converted into enantioenriched active agents: (R)-(-)-diprophylline (57% ee) and (S)-(+)-xanthinol nicotinate (65% ee). To support the assignment of absolute configurations of EKR-products as well as to confirm the stereochemical outcome of the remaining reaction steps, docking studies toward the prediction of enantiomers binding selectivity in CAL-B active site as well as the respective chemical correlations with enantiomerically enriched analytical standards obtained from commercially available (R)-(-)-epichlorohydrin, were applied. In addition, single-crystal X-ray diffraction (XRD) analyses were performed for the synthesized optically active APIs furnishing by this manner a first crystal structures of nicotinic acid salt of xanthinol.
Xanthinol Nicotinate in the management of leg ulcers associated with haemoglobinopathies
Curr Med Res Opin 1979;6(5):309-13.PMID:540521DOI:10.1185/03007997909109443.
The therapeutic role of Xanthinol Nicotinate, with its potent action on the peripheral circulation, in promoting healing of leg ulcers when added to conservative measures of ulcer treatment in adult beta-thalassaemia major and sickle cell thalassaemia, was evaluated in a double-blind crossover trial in 16 patients suffering from multiple leg ulcers. Conservative measures of ulcer treatment were leg raising in horizontal position for 14 hours, bed-rest, local antiseptic dressings and antibiotics. Xanthinol Nicotinate or placebo was administered in a daily dose of 8 tablets (2400 mg) for 10 weeks. Comparison of the treatment results of conservative measures plus Xanthinol Nicotinate and those of conservative measures plus placebo revealed a statistically significant higher rate of complete ulcer healing during Xanthinol Nicotinate therapy (p less than 0.01). Apart from a low incidence of generalized itching and flushing at the start of the trial, Xanthinol Nicotinate was well tolerated in the prescribed dose.
Development and validation of a liquid chromatography-tandem mass spectrometry method for the determination of xanthinol in human plasma and its application in a bioequivalence study of Xanthinol Nicotinate tablets
J Chromatogr B Analyt Technol Biomed Life Sci 2008 Sep 15;873(1):20-6.PMID:18718822DOI:10.1016/j.jchromb.2008.07.045.
A sensitive, rapid liquid chromatographic-electrospray ionization mass spectrometric method for the determination of xanthinol in human plasma was developed and validated. Xanthinol Nicotinate in plasma (0.5 mL) was pretreated with 20% trichloroacetic acid for protein precipitation. The samples were separated using a Lichrospher silica (5 microm, 250 mm x 4.6 mm i.d.). A mobile phase of methanol-water containing 0.1% formic acid (50: 50, v/v) was used isocratically eluting at a flow rate of 1 mL/min. Xanthinol and its internal standard (IS), acyclovir, were measured by electrospray ion source in positive selected reaction monitoring mode. The method demonstrated that good linearity ranged from 10.27 to 1642.8 ng/mL with r=0.9956. The limit of quantification for xanthinol in plasma was 10.27 ng/mL with good accuracy and precision. The mean plasma extraction recovery of xanthinol was in the range of 90.9-100.2%. The intra- and inter-batch variability values were less than 4.8% and 7.9% (relative standard deviation, R.S.D.), respectively. The established method has been successfully applied to a bioequivalence study of two Xanthinol Nicotinate tablets for 20 healthy volunteers.
The effects of nicotinic acid and Xanthinol Nicotinate on human memory in different categories of age. A double blind study
Psychopharmacology (Berl) 1985;87(4):390-5.PMID:3936095DOI:10.1007/BF00432500.
The treatment effect of nicotinic acid and Xanthinol Nicotinate on human memory was compared with placebo in 96 healthy subjects. Forty-three subjects were young (35-45 years), 30 subjects middle aged (55-65 years) and 23 subjects were old aged (75-85 years). Pre- and post-treatment scores were measured on a battery of memory tasks, covering sensory register, short-term memory and long-term memory. The treatment regime was 1 dragee t.i.d. for 8 weeks. The administration of Xanthinol Nicotinate (500 mg, containing 141.7 mg nicotinic acid), nicotinic acid (141.7 mg) and placebo (lactose) was double-blind. Pre- and post-treatment scores were analysed by means of a multivariate covariance technique, the pre-treatment score serving as covariate. Nicotinic acid treatment resulted in improvement of sensory register and short-term memory, while Xanthinol Nicotinate improved sensory register, short-term memory and long-term memory. In comparison with placebo, both active compounds yielded improvements of 10-40%, depending on type of task. Treatment effects of nicotinic acid were predominantly found in the young and middle-aged, whereas treatment effects of Xanthinol Nicotinate were predominantly found in the old. These results are interpreted by the supposed activity of nicotinic acid at the cell membrane, improving neuronal transmission, and of Xanthinol Nicotinate inside the cell, enhancing cell metabolism and oxygen supply in the brain.
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.PMID:19585554DOI:10.1002/ijc.24724.
The tumor micro-environment plays a key role in the tumor resistance to cytotoxic treatments. It has been demonstrated that it is possible to modulate the tumor microenvironment to potentiate anti-cancer therapy. Here, we made the hypothesis that the vasoactive agent Xanthinol Nicotinate (XN) could be an important modulator of the tumor perfusion and oxygenation. Using functional non invasive techniques (in vivo EPR oximetry and dynamic contrast enhanced MRI), we were able to define a time window in which tumor oxygenation, flow and permeability were significantly increased in the TLT tumor model implanted in muscles of mice. As a consequence of the alleviation of tumor hypoxia, we found out that XN was able to radiosensitize the tumors when applying 10 Gy of X-Rays during the reoxygenation of the tumors (enhancement in radiation response of 1.4). Moreover, the administration of cyclosphosphamide (50 mg/kg) used as a chemotherapeutic agent was more efficient when applying the treatment after XN administration (enhancement in response to chemotherapy of 2.7). These results show the importance of the dynamic evolution of the tumor microenvironment on the response to treatments, and that XN is an efficient modulator of the tumor hemodynamics that may potentiate cytotoxic treatments.