Nicotinamide (Synonyms: 煙酰an; Niacinamide; Nicotinic acid amide)
Nicotinamide 是wei生素 B3 或煙suan的一種形式，可抑制 SIRT2 的體外活性，其 EC50 值為 2 μM。 Nicotinamide 可抑制 90% 的黑色素瘤細(xì)胞數(shù)量，并增加細(xì)胞內(nèi) NAD+、ATP、ROS 水平。Nicotinamide 抑制黑色素瘤小鼠的腫瘤生長并提高生存率，可用于黑色素瘤等皮膚ai相關(guān)的研究。
生物活性
Nicotinamide is a form of vitamin B3 or niacin that inhibits sirtuin 2 (SIRT2) activity in vitro, with an EC50 of 2 μM. Nicotinamide inhibits up to 90% melanoma cell number and increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma[1].
體外研究(In Vitro)
Nicotinamide (0-50 mM, 24/48 h ) reduces cell number in a time-dependent and dose-dependent manner in A375 and SK-MEL-28 cells[1].
Nicotinamide (10-50 mM, 24 h ) makes A375 cells undergo accumulation in G1 phase, reduction in S phase, and increase inthe sub-G1 (apoptosis) phase[1].
Nicotinamide (1-50 mM, 6 h ) increases NAD+, ATP and ROS levels in A375 and SK-MEL-28 cells[1].
Nicotinamide (0.01-20 mM, 1 h) inhibits purified SIRT2 enzymatic activity in vitro with an EC50 of 2 μM[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
| Cell Line: | A375, SK-MEL-28, mouse B16-F10 cell |
| Concentration: | 0, 1, 20, 50 mM |
| Incubation Time: | |
| Result: | 24 h, 48 h |
體內(nèi)研究(In Vivo)
Nicotinamide (Intraperitoneal injection, 1500 and 1800 mg/Kg, 5 days per week) inhibits tumor growth in murine metastatic melanoma model[1].
Nicotinamide (Intraperitoneal injection, 1800 mg/Kg, once a day, murine metastatic melanoma model) affects IFN-γ (a key mediator of cell-mediated anti-tumor immunity), increases the plasma levels of eotaxin and IL-5, reduces the plasma levels of IL-3, IL-12, RANTES and IL-10[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6 mice (subcutaneous injected with B16-F10 cells)[1] |
| Dosage: | 1000, 1500, 1800 mg/Kg. |
| Administration: | Intraperitoneal injection, 5 days per week (followed by 2-day rest) or once a day. |
| Result: | Inhibited tumor growth at 1500 and 1800 mg/Kg, and had no effect on the body weight. Increased the frequency of IFN-γ producing cells and modulated the protein levels of cytokines and chemokines in the plasma of tumor-bearing mice. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04910061 | Seneque SA|Dicentra Inc.|LGD | August 5, 2021 | Not Applicable | |
| NCT05258474 | University Hospital Schleswig-Holstein | December 4, 2020 | Phase 1 | |
| NCT05194397 | Children′s Hospital of Philadelphia|National Institutes of Health (NIH)|City of Hope Medical Center|St. Jude Children′s Research Hospital|National Cancer Institute (NCI)|University of Pennsylvania | November 18, 2022 | Phase 2 |
分子量：122.12
性狀：Solid
Formula：C6H6N2O
CAS 號：98-92-0
中文名稱：煙酰an
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式：
4°C, protect from light
*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性數(shù)據(jù)
In Vitro:
DMSO : 50 mg/mL (409.43 mM; Need ultrasonic)
H2O : ≥ 50 mg/mL (409.43 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 8.1887 mL | 40.9433 mL | 81.8867 mL |
| 5 mM | 1.6377 mL | 8.1887 mL | 16.3773 mL |
| 10 mM | 0.8189 mL | 4.0943 mL | 8.1887 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： PBS
Solubility: 100 mg/mL (818.87 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (20.47 mM); Clear solution
參考文獻(xiàn)
[1]. [1] Francesca Scatozza, et al. Nicotinamide inhibits melanoma in vitro and in vivo. J Exp Clin Cancer Res. 2020 Oct 7;39(1):211. [Content Brief]
注：產(chǎn)品僅用于科研
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