TRIA-662 (1-Methylnicotinamide chloride)
(Synonyms: 3-氨基甲酰-1-甲基氯化吡啶,1-Methylnicotinamide chloride; N-methylnicotinamide chloride) 目录号 : GC42000
TRIA-662 (1-Methylnicotinamide chloride)是烟酰胺经烟酰胺N-甲基转移酶（NNMT）催化生成的主要代谢产物。
Cas No.:1005-24-9
Sample solution is provided at 25 µL, 10mM.
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TRIA-662 (1-Methylnicotinamide chloride) is the principal metabolite of nicotinamide generated by nicotinamide N-methyltransferase (NNMT)[1]. TRIA-662 exerts antithrombotic and anti-inflammatory effects by promoting prostacyclin release and improving nitric-oxide bioavailability[2]. TRIA-662 is commonly used as a fluorogenic probe substrate as well as food supplement ingredient[3][4].
In vitro, treatment of human dermal microvascular endothelial cells (HMECs) with TRIA-662(0.1μM; 3h) reduced TNF-α-induced increases in endothelial cell stiffness, induced slight F-actin depolymerization, and restored NO and PGI₂ levels toward baseline[5].
In vivo, TRIA-662 (100mg/kg/day; p.o.; 19 days)showed significant anti-metastasis activity, increased tumor angiogenesis,decreased the number of lung metastases and elevated the E-cadherin to N-cadherin expression ratio in the 4T1 tumor-bearing mouse model[6]. TRIA-662 (200µL;300mM; i.v.; 10min before hypoxic stress) reduced the hypoxia-induced cardiac injury biomarker troponin T levels, decreased creatine kinase activity, and increased myocardial phosphocreatine content and phosphocreatine/creatine ratio in ApoE-/-LDLr-/- mice without causing hypernatremia[7].
References:
[1] Wozniacka A, Wieczorkowska M, Gebicki J, Sysa-Jedrzejowska A. Topical application of 1-methylnicotinamide in the treatment of rosacea: a pilot study. Clin Exp Dermatol. 2005;30(6):632-635.
[2] Szafarz M, Kus K, Walczak M, et al. Pharmacokinetic Profile of 1-Methylnicotinamide Nitrate in Rats. J Pharm Sci. 2017;106(5):1412-1418.
[3] Elokely KM, Eldawy MA, Elkersh MA, El-Moselhy TF. Fluorescence Spectrometric Determination of Drugs Containing α-Methylene Sulfone/Sulfonamide Functional Groups Using N-Methylnicotinamide Chloride as a Fluorogenic Agent. Int J Anal Chem. 2011;2011:840178.
[4] EFSA Panel on Dietetic Products, Nutrition and Allergies (NDA), Turck D, Bresson JL, et al. Safety of 1-methylnicotinamide chloride (1-MNA) as a novel food pursuant to Regulation (EC) No 258/97. EFSA J. 2017;15(10):e05001.
[5] Kolodziejczyk AM, Brzezinka GD, Khurana K, Targosz-Korecka M, Szymonski M. Nanomechanical sensing of the endothelial cell response to anti-inflammatory action of 1-methylnicotinamide chloride. Int J Nanomedicine. 2013;8:2757-2767.
[6] Blazejczyk A, Switalska M, Chlopicki S, et al. 1-methylnicotinamide and its structural analog 1,4-dimethylpyridine for the prevention of cancer metastasis. J Exp Clin Cancer Res. 2016;35(1):110.
[7] Zabielska MA, Adamus J, Kowalski R, et al. Cardioprotective effect of N-methylnicotinamide salt of pyruvate in experimental model of cardiac hypoxia. Pharmacol Rep. 2018;70(2):378-384.
TRIA-662 (1-Methylnicotinamide chloride)是烟酰胺经烟酰胺N-甲基转移酶（NNMT）催化生成的主要代谢产物[1]。TRIA-662通过促进前列环素释放及改善一氧化氮生物利用度，具有抗血栓和抗炎作用[2]。TRIA-662常用作荧光探针底物以及食品补充剂成分[3][4]。
在体外实验中，以0.1µM浓度处理人微血管内皮细胞（HMECs）3小时，TRIA-662显著降低了TNF-α诱导的细胞弹性增加，诱导F-肌动蛋白轻微解聚，并使NO和PGI₂水平恢复至接近正常水平[5]。
在体内实验中，TRIA-662（100mg/kg/天；口服；19天）在4T1肿瘤小鼠模型中显示出显著的抗转移活性，增加了肿瘤血管生成，减少了肺部转移灶数量，并提高了E-钙粘蛋白与N-钙粘蛋白的表达比值[6]。TRIA-662（200µL；300mM；静脉注射；缺氧应激前10分钟）降低ApoE-/-LDLr-/-小鼠缺氧诱导的心脏损伤生物标志物肌钙蛋白T水平，降低肌酸激酶活性，增加心肌磷酸肌酸含量和磷酸肌酸/肌酸比值，而不引起高钠血症[7]。
| Cell experiment [1]: | |
Cell lines | human dermal microvascular endothelial cells (HMECs) |
Preparation Method | Human dermal microvascular endothelial cells (HMECs) were cultured in MCDB medium supplemented with 10% serum, 1% L-glutamine, 2% hydrocortisone, 0.001% epidermal growth factor, and 0.1% antibiotics (penicillin, streptomycin, and fungisan). Cells were exposed to 10ng/mL TNF-α for 1h and then incubated with 0.1μM TRIA-662 for 3h. The cells exposed to TNF-α only were used as a reference for the combined samples (TNF-α and TRIA-662) for the corresponding incubation period. The elasticity, NO production, and fluorescent staining of the actin cytoskeleton were investigated to determine the therapeutic behavior of TRIA-662. |
Reaction Conditions | 0.1μM; 3h |
Applications | TRIA-662 reduced TNF-α-induced increases in endothelial cell stiffness, induced slight F-actin depolymerization, and restored NO and PGI₂ levels toward baseline in HMECs. |
| Animal experiment [2]: | |
Animal models | apolipoprotein E-deficient/LDL receptor-deficient (ApoE-/-LDLr-/- ) mice |
Preparation Method | Male apolipoprotein E-deficient/LDL receptor-deficient (ApoE-/-LDLr-/- ) mice were housed in 12h/12h light/dark cycle in temperature controlled cages (24°C, 40% humidity) and they had an unlimited access to water and standard chow diet. For experiments, 7-month-old male animals were used randomly divided into 3 or 4 groups. At 10min before hypoxic stress, under anaesthesia one group of mice was intravenously injected with a 200µl 300mM bolus dose of sodium pyruvate, second with TRIA-662 pyruvate, third with TRIA-662 and fourth with 0.9% sodium chloride as a control (n=4-7). The blood was collected by cardiac puncture and for the measurements at 2.5min, 5min, 7.5min and 10min different animals were used. Hearts were frozen in liquid nitrogen immediately after collection for further analyses. |
Dosage form | 200µL; 300mM; i.v.; 10min before hypoxic stress |
Applications | TRIA-662 reduced the hypoxia-induced cardiac injury biomarker troponin T levels, decreased creatine kinase activity, and increased myocardial phosphocreatine content and phosphocreatine/creatine ratioin ApoE-/-LDLr-/- mice without causing hypernatremia. |
References: | |
| 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 |
| 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 | 5.7937 mL | 28.9687 mL | 57.9374 mL |
| 5 mM | 1.1587 mL | 5.7937 mL | 11.5875 mL |
| 10 mM | 579.4 μL | 2.8969 mL | 5.7937 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 |
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| % 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。
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2.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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