1. PI3K/Akt/mTOR Autophagy Apoptosis
  2. PI3K Akt mTOR Autophagy Apoptosis
  3. Veratramine

Veratramine  (Synonyms: 黎芦碱; NSC17821; NSC23880)

目录号: HY-N0837 纯度: 99.84%
COA 产品使用指南 技术支持

Veratramine (NSC17821; NSC23880) 是一种口服有效的 PI3K/Akt/mTOR 信号通路抑制剂及 SIGMAR1 调节剂。Veratramine 诱导肿瘤细胞自噬性凋亡 (autophagy),阻滞细胞周期于 G0/G1 期,并抑制上皮-间质转化 (EMT) 相关蛋白减少肿瘤迁移。Veratramine 通过抑制 SIGMAR1 与 NMDAR 结合及 NMDAR Ser896 位点磷酸化,减轻神经病变模型中脊髓和坐骨神经病理损伤。Veratramine 具有抗肿瘤增殖、诱导凋亡 (apoptosis、抑制炎症及神经保护活性,可用于肝癌、骨肉瘤等癌症及糖尿病周围神经病变的研究。

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Veratramine Chemical Structure

Veratramine Chemical Structure

CAS No. : 60-70-8

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy[1][2][3][4].

体外研究
(In Vitro)

Veratramine (2.5-80 μM;24-72 h) 在人肝癌 HepG2 细胞实验中抑制细胞增殖、迁移及侵袭,诱导 G0/G1 期阻滞和自噬性凋亡,下调 PI3K/Akt/mTOR 信号通路相关蛋白[1]
Veratramine (30-50 μM;24-48 h) 在人骨肉瘤 143B 和 HOS 细胞实验中抑制细胞活力、迁移及侵袭,诱导细胞凋亡,下调 p-PI3K、p-Akt 及 EMT 相关蛋白 N-钙黏蛋白、波形蛋白[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HepG2 liver cancer cells
Concentration: 10, 20, 40 μM
Incubation Time: 48 h
Result: Flow cytometry revealed a dose-dependent increase in apoptotic cells (Annexin V+), with the highest apoptosis rate (51.86%) at 40 μM.
Cell cycle analysis showed G0/G1 phase arrest, with a significant reduction in S phase cells at 40 μM.

Western Blot Analysis[1]

Cell Line: HepG2 liver cancer cells
Concentration: 0, 10, 20, 40 μM
Incubation Time: 48 h
Result: Downregulated p-PI3K, p-Akt, and p-mTOR, and upregulated autophagy markers Beclin-1 and LC3-II/I.
Pro-apoptotic protein Bax was increased, while anti-apoptotic Bcl-2 was decreased.

Cell Migration Assay [2]

Cell Line: 143B and HOS osteosarcoma cells
Concentration: 0, 30, 40, 50 μM
Incubation Time: 24-48 h
Result: Wound healing and Transwell assays showed reduced migration and invasion at 40 μM and 50 μM.

Western Blot Analysis[2]

Cell Line: 143B and HOS osteosarcoma cells
Concentration: 0, 30, 40, 50 μM
Incubation Time: 24-48 h
Result: Western blot revealed decreased N-cadherin, Snail, vimentin, and MMP-2, indicating inhibition of epithelial-mesenchymal transition (EMT).
体内研究
(In Vivo)

Veratramine (2 mg/kg;尾静脉注射;每周 3 次;4 周) 抑制 BALB/c 裸鼠的肝癌皮下移植模型的肿瘤生长,降低肿瘤重量,无明显全身毒性[1]
Veratramine (20-40 mg/kg;口服灌胃;每 2 天 1 次;21 天) 减少 BALB/c 裸鼠骨肉瘤原位模型的肿瘤荧光信号强度,抑制肿瘤生长,对小鼠体重无显著影响[2]
Veratramine (50 μg/kg;尾静脉注射;每天 1 次;4 周) 提高 Sprague-Dawley 大鼠的糖尿病周围神经病变模型的机械痛阈值,延长冷热刺激耐受时间,减轻脊髓和坐骨神经病理损伤[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c Nude Mouse Hepatocellular Carcinoma Model (female, 16-18 g, 4-6 weeks old): subcutaneous hepatocellular carcinoma xenografts (HepG2 cells)[1]
Dosage: 2 mg/kg
Administration: Tail vein injection, 3 times a week for 4 weeks
Result: Significantly decreased the tumor volume was smaller compared to the control group. Reduced the average tumor weight.
There were no significant differences in body weight, food intake, or water intake between the two groups.
Led to a decrease in the number of proliferating cells and an increase in apoptotic cells in the tumor tissue in Histopathological examination.
Animal Model: BALB/c Nude Mouse Osteosarcoma Model (female, 25 g, 6 weeks old): orthotopic osteosarcoma xenografts (143B cells)[2]
Dosage: 20 mg/kg or 40 mg/kg
Administration: Oral gavage, every 2 days for 21 days
Result: Significantly lowered fluorescence intensity of the tumors than that in the control group, indicating reduced tumor growth.
Remained the body weight of the mice in all groups stable throughout the experiment.
Downregulated the expression of p-Akt and PCNA in the tumor tissue in Immunohistochemical analysis.
Animal Model: Sprague-Dawley Rat Diabetic Peripheral Neuropathy Model (male, 260-300 g, 8 weeks old): Streptozotocin-induced diabetic peripheral neuropathy[3]
Dosage: 50 µg/kg
Administration: Tail vein injection, once a day for 4 weeks
Result: Significantly increased he mechanical pain threshold and cold/hot stimulus tolerance time compared to the diabetic control group.
Resulted the spinal cord and sciatic nerve less damage in Histological examination.
Downregulated the expression of p-mTOR and p-4E-BP1 in the spinal cord and sciatic nerve tissues.
分子量

409.60

Formula

C27H39NO2

CAS 号
性状

固体

颜色

White to off-white

中文名称

黎芦碱;黎芦胺;藜芦铵

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (244.14 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4414 mL 12.2070 mL 24.4141 mL
5 mM 0.4883 mL 2.4414 mL 4.8828 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.10 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.10 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.84%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4414 mL 12.2070 mL 24.4141 mL 61.0352 mL
5 mM 0.4883 mL 2.4414 mL 4.8828 mL 12.2070 mL
10 mM 0.2441 mL 1.2207 mL 2.4414 mL 6.1035 mL
15 mM 0.1628 mL 0.8138 mL 1.6276 mL 4.0690 mL
20 mM 0.1221 mL 0.6104 mL 1.2207 mL 3.0518 mL
25 mM 0.0977 mL 0.4883 mL 0.9766 mL 2.4414 mL
30 mM 0.0814 mL 0.4069 mL 0.8138 mL 2.0345 mL
40 mM 0.0610 mL 0.3052 mL 0.6104 mL 1.5259 mL
50 mM 0.0488 mL 0.2441 mL 0.4883 mL 1.2207 mL
60 mM 0.0407 mL 0.2035 mL 0.4069 mL 1.0173 mL
80 mM 0.0305 mL 0.1526 mL 0.3052 mL 0.7629 mL
100 mM 0.0244 mL 0.1221 mL 0.2441 mL 0.6104 mL
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