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1-Methylnicotinamide (chloride) Sale

(Synonyms: 3-氨基甲酰-1-甲基氯化吡啶,1-Methylnicotinamide chloride; N-methylnicotinamide chloride) 目录号 : GC42000

A metabolite of nicotinamide

1-Methylnicotinamide (chloride) Chemical Structure

Cas No.:1005-24-9

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100mg
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产品描述

Nicotinamide is a precursor of NAD and NADP , which serve essential functions in modulating cellular redox status and controlling signaling and transcriptional events. 1-Methylnicotinamide (MNA) is a primary metabolite of nicotinamide produced by the action of nicotinamide N-methyltransferase . It demonstrates antithrombotic and anti-inflammatory properties through direct action on the endothelium by a mechanism involving the prostacyclin pathway and by improving nitric oxide bioavailability. Aggressive cancer cell lines are reported to have higher levels of MNA due to increased NNMT-directed transfer of methyl groups from S-adenosyl-L-methionine to nicotinamide, implicating a role for MNA in cancer cell metabolism.

Chemical Properties

Cas No. 1005-24-9 SDF
别名 3-氨基甲酰-1-甲基氯化吡啶,1-Methylnicotinamide chloride; N-methylnicotinamide chloride
Canonical SMILES NC(C1=CC=C[N+](C)=C1)=O.[Cl-]
分子式 C7H9N2O•Cl 分子量 172.6
溶解度 10mg/ml in PBS (pH 7.2) 储存条件 Store at -20°C
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1 mM 5.7937 mL 28.9687 mL 57.9374 mL
5 mM 1.1587 mL 5.7937 mL 11.5875 mL
10 mM 0.5794 mL 2.8969 mL 5.7937 mL
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Research Update

Safety of 1-Methylnicotinamide chloride (1-MNA) as a novel food pursuant to Regulation (EC) No 258/97

EFSA J 2017 Oct 26;15(10):e05001.PMID:32625296DOI:10.2903/j.efsa.2017.5001.

Following a request from the European Commission, the EFSA Panel on Dietetic Products, Nutrition and Allergies (NDA) was asked to deliver an opinion on 1-Methylnicotinamide chloride (1-MNA) as a novel food (NF) ingredient submitted pursuant to Regulation (EC) No 258/97 of the European Parliament and of the Council, taking into account the comments and objections of a scientific nature raised by Member States. 1-MNA is a substance present naturally in the human body as a normal downstream product of niacin metabolism. The Panel considers that the information provided on the composition, the specification and the batch-to-batch variability of the NF is sufficient. The applicant intends to use 1-MNA in food supplements and proposes a maximum intake of 58 mg/day. 1-MNA is not genotoxic. In a subchronic rat study, epithelium degeneration of the non-glandular stomach was observed at all dose levels with increasing frequency. The Panel notes that the human stomach does not have non-glandular epithelium and considers this finding is toxicologically not relevant for humans. At doses of 500 and 1,000 mg/kg body weight (bw), changes of the urine pH, that did not reverse in the recovery period, were reported. As adversity of this finding cannot be ruled out, the Panel selected 250 mg/kg bw in this rat study as the reference point. The Margin of Exposure to humans weighing 70 kg and consuming 58 mg would be about 300. The Panel notes the upper level for nicotinamide, i.e. 900 mg/day for adults. Taking into account that 1-MNA is a main metabolite from nicotinamide, the Panel considers that it is unlikely that an intake of 58 mg 1-MNA from food supplements would result in adverse health outcomes in humans. The Panel concludes that the NF, 1-MNA, is safe under the proposed uses and use levels.

1-Methylnicotinamide and its structural analog 1,4-dimethylpyridine for the prevention of cancer metastasis

J Exp Clin Cancer Res 2016 Jul 13;35(1):110.PMID:27412454DOI:10.1186/s13046-016-0389-9.

Background: 1-Methylnicotinamide (1-MNA), an endogenous metabolite of nicotinamide, has recently gained interest due to its anti-inflammatory and anti-thrombotic activities linked to the COX-2/PGI2 pathway. Given the previously reported anti-metastatic activity of prostacyclin (PGI2), we aimed to assess the effects of 1-MNA and its structurally related analog, 1,4-dimethylpyridine (1,4-DMP), in the prevention of cancer metastasis. Methods: All the studies on the anti-tumor and anti-metastatic activity of 1-MNA and 1,4-DMP were conducted using the model of murine mammary gland cancer (4T1) transplanted either orthotopically or intravenously into female BALB/c mouse. Additionally, the effect of the investigated molecules on cancer cell-induced angiogenesis was estimated using the matrigel plug assay utilizing 4T1 cells as a source of pro-angiogenic factors. Results: Neither 1-MNA nor 1,4-DMP, when given in a monotherapy of metastatic cancer, influenced the growth of 4T1 primary tumors transplanted orthotopically; however, both compounds tended to inhibit 4T1 metastases formation in lungs of mice that were orthotopically or intravenously inoculated with 4T1 or 4T1-luc2-tdTomato cells, respectively. Additionally, while 1-MNA enhanced tumor vasculature formation and markedly increased PGI2 generation, 1,4-DMP did not have such an effect. The anti-metastatic activity of 1-MNA and 1,4-DMP was further confirmed when both agents were applied with a cytostatic drug in a combined treatment of 4T1 murine mammary gland cancer what resulted in up to 80 % diminution of lung metastases formation. Conclusions: The results of the studies presented below indicate that 1-MNA and its structural analog 1,4-DMP prevent metastasis and might be beneficially implemented into the treatment of metastatic breast cancer to ensure a comprehensive strategy of metastasis control.

Pharmacokinetic Profile of 1-Methylnicotinamide Nitrate in Rats

J Pharm Sci 2017 May;106(5):1412-1418.PMID:28153597DOI:10.1016/j.xphs.2017.01.022.

Treatment with 1-Methylnicotinamide (MNA), a major metabolite of nicotinamide, exerts antithrombotic, anti-inflammatory, and vasoprotective effects. Yet, pharmacokinetic (PK) profile of MNA has not been fully characterized. In the present work, we analyze the PK profile of the MNA given as a nitrate (MNANO3) in comparison to nitrite (MNANO2) or chloride (MNACl) in rats. The bioavailability of MNA administered as MNANO3 equaled 22.4% as compared to MNANO2 or MNACl (9.2% and 9.1%, respectively). Moreover, in single-pass intestinal perfusion experiments, effective permeability of MNA given as MNANO3 was higher as compared to MNA administered as MNANO2 or MNACl. In turn, tmax was the shortest and Cmax the highest (0.22 h and 56.65μM) for intragastrically administered MNANO2 comparing to MNANO3 (1.92 h, 21.74μM) or MNACl (0.63 h, 16.13μM). Transfer constant between central and peripheral compartments (kcp) and volume of distribution (Vss) for MNANO3 (0.33 h-1 and 1.96 L/kg) were higher as compared to MNANO2 or MNACl (0.11 h-1, 0.08 h-1 for kcp and 1.05 L/kg, 0.76 L/kg for Vss, respectively). In conclusion, we characterized PK profile of MNA and demonstrated that nitrate ion augmented bioavailability and favorably modified PK profile of MNA. Furthermore, given vasoprotective properties of MNA as well as nitrate, MNANO3 represents a bifunctional compound.

Nanomechanical sensing of the endothelial cell response to anti-inflammatory action of 1-Methylnicotinamide chloride

Int J Nanomedicine 2013;8:2757-67.PMID:23946648DOI:10.2147/IJN.S46936.

Background: There is increasing evidence that cell elastic properties should change considerably in response to chemical agents affecting the physiological state of the endothelium. In this work, a novel assay for testing prospective endothelium-targeted agents in vitro is presented. Materials and methods: The proposed methodology is based on nanoindentation spectroscopy using an atomic force microscope tip, which allows for quantitative evaluation of cell stiffness. As an example, we chose a pyridine derivative, 1-Methylnicotinamide chloride (MNA), known to have antithrombotic and anti-inflammatory properties, as reported in recent in vivo experiments. Results: First, we determined a concentration range of MNA in which physiological parameters of the endothelial cells in vitro are not affected. Then, cell dysfunction was induced by incubation with tumor necrosis factor-alpha (TNF-α) and the cellular response to MNA treatment after TNF-α incubation was studied. In parallel to the nanoindentation spectroscopy, the endothelium phenotype was characterized using a fluorescence spectroscopy with F-actin labeling, and biochemical methods, such as secretion measurements of both nitric oxide (NO), and prostacyclin (PGI2) regulatory agents. Conclusion: We found that MNA could reverse the dysfunction of the endothelium caused by inflammation, if applied in the proper time and to the concentration scheme established in our investigations. A surprisingly close correlation was found between effective Young's modulus of the cells and actin polymerization/depolymerization processes in the endothelium cortical cytoskeleton, as well as NO and PGI2 levels. These results allow us to construct the physiological model of sequential intracellular pathways activated in the endothelium by MNA.

Topical application of 1-Methylnicotinamide in the treatment of rosacea: a pilot study

Clin Exp Dermatol 2005 Nov;30(6):632-5.PMID:16197374DOI:10.1111/j.1365-2230.2005.01908.x.

Rosacea is a chronic facial dermatosis with a progressive course, which is characterized by the presence of erythema, papules, pustules, telangiectasias and sebaceous gland hyperplasia. However, the aetiology is still unknown; genetic predisposition, gastrointestinal disorders (Helicobacter pylori), infestations with Demodex folliculorum and environmental stimuli are considered to be involved in the inflammatory process. A metabolite of nicotinamide, 1-Methylnicotinamide (MNA(+)), has anti-inflammatory properties, and this is the first study to test the effectiveness of this agent in treating rosacea. In total, 34 patients with rosacea were treated with a gel containing 0.25% MNA(+) as a chloride salt, twice daily for 4 weeks, after which improvement was observed in 26/34 cases. The improvement was good in 9/34 and moderate in 17/34, but no clinical effect was noted in seven subjects. In only one case was skin irritation given as the reason for treatment withdrawal. These results indicate that MNA(+) might be a useful agent for treating rosacea.