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

Veratramine  (Synonyms: NSC17821; NSC23880)

Cat. No.: HY-N0837 Purity: 99.84%
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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.

For research use only. We do not sell to patients.

Veratramine Chemical Structure

Veratramine Chemical Structure

CAS No. : 60-70-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Veratramine:

Veratramine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Veratramine

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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View All Isoforms
Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

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].

In Vitro

Veratramine (2.5-80 μM; 24-72 h) inhibits cell proliferation, migration and invasion, induces G0/G1 arrest and autophagic apoptosis, and downregulates proteins related to the PI3K/Akt/mTOR signaling pathway in human hepatoma HepG2 cell experiments[1].
Veratramine (30-50 μM; 24-48 h) inhibits cell viability, migration and invasion, induces apoptosis, and downregulates p-PI3K, p-Akt, and EMT-related proteins N-cadherin and vimentin in human osteosarcoma 143B and HOS cell experiments[2].

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

Veratramine Related Antibodies

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).
In Vivo

Veratramine (2 mg/kg; tail vein injection; 3 times a week; 4 weeks) inhibits tumor growth and reduces tumor weight in the subcutaneous transplant model of liver cancer in BALB/c nude mice, without obvious systemic toxicity[1].
Veratramine (20-40 mg/kg; oral gavage; once every 2 days; 21 days) reduces the tumor fluorescence signal intensity and inhibits tumor growth in the orthotopic model of osteosarcoma in BALB/c nude mice, without significant effect on mouse body weight[2].
Veratramine (50 μg/kg; tail vein injection; once a day; 4 weeks) increases the mechanical pain threshold in the diabetic peripheral neuropathy model of Sprague-Dawley rats, prolongs the tolerance time to cold and hot stimuli, and reduces the pathological damage of the spinal cord and sciatic nerve[3].

MedChemExpress (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.
Molecular Weight

409.60

Formula

C27H39NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H]([C@H](C2=C(C)C3=C(C=C2)[C@]4([H])CC=C(C[C@@H](O)CC5)[C@@]5(C)[C@@]4([H])C3)C)NC[C@@H](C)C1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (244.14 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.84%

SDS (393 KB)

COA (251 KB) LCMS (86 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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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Veratramine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Veratramine60-70-8NSC17821 NSC23880NSC 17821NSC-17821NSC23880NSC 23880NSC-23880PI3KAktmTORAutophagyApoptosisPhosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinInhibitorinhibitorinhibit

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