生物活性

Nicotinamide is a NAD+ and NADP+ coenzyme precursor. Nicotinamide is an antiinflammatory agent and a PARP-1 enzyme inhibitor.Promotes differentiation of mesenchymal stem cells to insulin producing cells when used in combination with growth factors and high glucose concentration.

IC50 (mM) values of nicotinamide on T. cruzi epimastigotes[1]

Inhibition of SIRT3/SIRT1 by nicotinamide[2]

体外研究

体内研究

激酶实验

Measurementof IC50Values for nicotinamide (NAM)[2]

This assay was used to measure the potencyof inhibition of SIRT3 and SIRT1 by NAM, and isoNAM. Reactions were performedin the presence of 100 mM NAD+, and either NAM (0, 1, 5, 10, 50,100, 200, 500 mM) or isoNAM (0, 0.05, 0.1, 1, 5, and 10 mM). The initial rateswere measured at different concentrations of NAM and isoNAM, and the reactionconditions were the same as above. The data were fitted to equation below byusing Prism to calculate the IC50 values: vi=v0{1-1/(IC50+[I] )} where v0is the initial rate of the uninhibited reaction andviis the initial rate of the reaction at concentration I of theinhibitor.

细胞实验

Proliferationassays[3]

Cell were labeled with CFSE and incubatedwith CpG/IL-2. Nicotinamide (1.2–10 mmol/L dose range) was added at thebeginning of culture. Proliferation was measured after 5 days by staining withanti-CD19PE. Cells were analyzed by flow cytometry, by using a fluorescence-activatedcell sorting CantoII equipment and the Diva and WinMDI softwares. Cellproliferation was also measured by [3H]-thymidine incorporation atday 5. The percentage of proliferating cells was calculated as [(number ofproliferated cells/total number of cells) x 100].

动物实验

Animalcare[4]

Male OLETF rats were provided. The ratswere maintained in a temperature- and humidity-controlled room on a 12 hlight/dark cycle and fed standard irradiated rodent chow (5% wt/wt fat) withunlimited access to food and water. Thirty rats, at approximately 28 weeks ofage, were divided into five groups: (1) HF diet (45% calories from fat; n=8),(2) HF diet and 10 mg nicotinic acid (NA)/kg body weight (BW)/day (NA 10; n=5),(3) HF diet and 100 mg NA/kg BW/day (NA 100; n=4), (4) HF diet and 10 mgnicotinamide (NAM) /kg BW/day (NAM 10; n=5), and (5) HF diet and 100 mg NAM/kgBW/day (NAM 100; n=8). NA and NAM were delivered via drinking water.

Oralglucose tolerance test (OGTT)

After a 16 h fast, glucose solutions weregiven via stomach gavage (2 g/kg). Blood glucose levels were measured at 0, 15,30, 60, 90, and 120 min after the glucose challenge using a Glucocard X-Meter.

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Soares MB, Silva CV, Bastos TM, et al. Anti-Trypanosoma cruzi activity of nicotinamide. Acta Trop. 2012;122(2):224-229.
[2] Guan X, Lin P, Knoll E, Chakrabarti R. Mechanism of inhibition of the human sirtuin enzyme SIRT3 by nicotinamide: computational and experimental studies. PLoS One. 2014;9(9):e107729.
[more]

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

相关化合物库

使用AMQUAR产品发表文献后请联系我们