2. Immunology/Inflammation NF-κB MAPK/ERK Pathway Stem Cell/Wnt
  3. AP-1 NF-κB p38 MAPK ERK JNK
  4. Armepavine

Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia.

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Armepavine

Armepavine Chemical Structure

CAS No. : 524-20-9

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Armepavine:

Armepavine Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Armepavine, found in Nelumbo nucifera, is an orally active NF-κB inhibitor. Armepavine attenuates expression of p-p65, α-SMA, p-JNK1/2, p-ERK1/2, p-p38α stimulated by TNF-α and LPS. Armepavine suppresses NF-κB nuclear translocation, IκBα phosphorylation, and collagen deposition. Armepavine can be used for the research of hepatic fibrosis and leukemia[1][2].

IC50 & Target[1]

p65

 

NF-κB

 

p38 MAPK

 

ERK1

 

ERK2

 

JNK

 

In Vitro

Armepavine (1-10 μM; 24 h) does not exert cytotoxic effects on HSC-T6 rat hepatic stellate cells[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α-induced collagen deposition in HSC-T6 rat hepatic stellate cells, with significant inhibition at 10 μM[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF−α- and LPS-induced α-SMA protein expression in HSC-T6 rat hepatic stellate cells[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α- and LPS-induced AP-1 transcriptional activity in HSC-T6 rat hepatic stellate cells, with significant effects at 10 μM for TNF-α and 3-10 μM for LPS[1].
Armepavine (1-10 μM; 6 h) concentration-dependently inhibits TNF-α-induced IκBα phosphorylation and NFκB p65 nuclear translocation in HSC-T6 rat hepatic stellate cells[1].
Armepavine (1-10 μM; 6 h) concentration-dependently inhibits TNF-α-induced NFκB transcriptional activity in HSC-T6 rat hepatic stellate cells, with significant effects at 1 and 10 μM[1].
Armepavine (10 μM; 15-60 min) inhibits TNF-α-induced phosphorylation of p38, ERK1/2, and JNK1/2 in HSC-T6 rat hepatic stellate cells[1].
Armepavine (1-10 μM; 24 h) concentration-dependently inhibits TNF-α-induced mRNA expression of iNOS, collagen 1α2, TIMP-1, and α-SMA in HSC-T6 rat hepatic stellate cells[1].

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

Armepavine Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: rat hepatic stellate cell line HSC-T6
Concentration: 1 μM; 3 μM; 10 μM
Incubation Time: 24 h
Result: Did not reduce HSC-T6 cell viability, with viability measured at 98% of untreated controls, showing no significant difference from controls.
Showed no cytotoxicity across the concentration range of 1-10 μM.

Western Blot Analysis[1]

Cell Line: rat hepatic stellate cell line HSC-T6 stimulated with TNF-α or LPS
Concentration: 1 μM; 3 μM; 10 μM
Incubation Time: 24 h
Result: Reduced TNF-α-stimulated α-SMA expression to 160%, 127%, and 106% of control levels at 1, 3, and 10 μM respectively.
Reduced LPS-stimulated α-SMA expression in a concentration-dependent manner across 1-10 μM.

Western Blot Analysis[1]

Cell Line: rat hepatic stellate cell line HSC-T6 stimulated with TNF-α
Concentration: 1 μM; 3 μM; 10 μM
Incubation Time: 6 h
Result: Reduced TNF-α-increased cytoplasmic IκBα phosphorylation and nuclear NFκB p65 protein levels in a concentration-dependent manner across 1-10 μM, with significant inhibition observed at 3 and 10 μM.

Western Blot Analysis[1]

Cell Line: rat hepatic stellate cell line HSC-T6 stimulated with TNF-α
Concentration: 10 μM
Incubation Time: 15 min; 30 min; 60 min
Result: Significantly attenuated the TNF-α-induced phosphorylation of ERK1/2 at 15 minutes, p38 at 30 minutes, and JNK1/2 at 60 minutes.

Real Time qPCR[1]

Cell Line: rat hepatic stellate cell line HSC-T6 stimulated with TNF-α
Concentration: 1 μM; 3 μM; 10 μM
Incubation Time: 24 h
Result: Reduced TNF-α-stimulated mRNA expression of iNOS, collagen 1α2, TIMP-1, and α-SMA in a concentration-dependent manner across 1-10 μM, with significant inhibition observed at 3 and 10 μM for most genes.
In Vivo

Armepavine (3-10 mg/kg; p.o.; twice daily; 3 weeks) exerts dose-dependent anti-hepatic fibrosis effects in bile duct-ligated rats, with the 10 mg/kg dose reducing fibrosis scores by 47% and collagen content to 4.38 mg/g liver, and the 3 mg/kg dose reducing fibrosis scores by 24% and hepatocyte necrosis scores by 68%[1].

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

Animal Model: Sprague-Dawley (male, 250~300 g, bile duct ligation-induced hepatic fibrosis)[1]
Dosage: 3 mg/kg; 10 mg/kg
Administration: p.o.; twice daily; 3 weeks
Result: Increased body weight to 333 g, reduced liver weight to 27.5 g, decreased plasma ALT to 536 U/L and AST to 127 U/L, reduced fibrosis score to 1.85 (24% reduction from vehicle-treated BDL rats), reduced hepatocyte necrosis score to 0.38 (68% reduction from vehicle-treated BDL rats), reduced hepatic mRNA expression of col 1α2 to 7.45, TGF-β1 to 14.5, TIMP-1 to 4.36, ICAM-1 to 15.5, and IL-6 to 10.5 relative to GAPDH.
Increased body weight to 345 g, reduced liver weight to 26.3 g, decreased plasma ALT to 434 U/L and AST to 73 U/L, reduced hepatic collagen content to 4.38 mg/g liver, reduced α-SMA/α-tubulin ratio to 141%, reduced fibrosis score to 1.28 (47% reduction from vehicle-treated BDL rats), reduced hepatocyte necrosis score to 0.50 (57% reduction from vehicle-treated BDL rats), reduced hepatic mRNA expression of col 1α2 to 5.09, TGF-β1 to 7.09, TIMP-1 to 3.87, ICAM-1 to 7.03, iNOS to 3.09, and IL-6 to 4.09 relative to GAPDH; increased hepatic metallothionein mRNA expression to 0.57 relative to GAPDH.
Molecular Weight

313.39

Formula

C19H23NO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C=C1)=CC=C1C[C@@H]2C3=CC(OC)=C(OC)C=C3CCN2C
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (319.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1909 mL 15.9546 mL 31.9091 mL
5 mM 0.6382 mL 3.1909 mL 6.3818 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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Concentration (final)

C2

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Volume (final)

V2

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 (7.98 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 (7.98 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:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.53%

SDS (252 KB)

COA (249 KB) HNMR (150 KB) RP-HPLC (74 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1909 mL 15.9546 mL 31.9091 mL 79.7728 mL
5 mM 0.6382 mL 3.1909 mL 6.3818 mL 15.9546 mL
10 mM 0.3191 mL 1.5955 mL 3.1909 mL 7.9773 mL
15 mM 0.2127 mL 1.0636 mL 2.1273 mL 5.3182 mL
20 mM 0.1595 mL 0.7977 mL 1.5955 mL 3.9886 mL
25 mM 0.1276 mL 0.6382 mL 1.2764 mL 3.1909 mL
30 mM 0.1064 mL 0.5318 mL 1.0636 mL 2.6591 mL
40 mM 0.0798 mL 0.3989 mL 0.7977 mL 1.9943 mL
50 mM 0.0638 mL 0.3191 mL 0.6382 mL 1.5955 mL
60 mM 0.0532 mL 0.2659 mL 0.5318 mL 1.3295 mL
80 mM 0.0399 mL 0.1994 mL 0.3989 mL 0.9972 mL
100 mM 0.0319 mL 0.1595 mL 0.3191 mL 0.7977 mL
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Armepavine 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:

Armepavine524-20-9AP-1NF-κBp38 MAPKERKJNKActivator Protein 1Nuclear factor-κBNuclear factor-kappaBExtracellular signal regulated kinasesc-Jun N-terminal kinasebile duct-ligated ratsERK1/2hepatic stellate cellsHSC-T6 rat hepatic stellate cellscaspase-3Bcl-2Inhibitorinhibitorinhibit

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