Art. -Nr.: HY-N6857

Armepavine

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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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Reinheit: 99.19%
CAS. Nr.: 524-20-9
Formel: C₁₉H₂₃NO₃
Molecular Weight:313.39

Speicherung:

4°C, protect from light

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

Armepavine Chemical Structure

CAS. Nr.: 524-20-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

p65

NF-κB

p38 MAPK

ERK1

ERK2

JNK

Alle AP-1 Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

Alle JNK Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 524-20-9
Appearance Solid
Molecular Weight 313.39
Formel C₁₉H₂₃NO₃
Color White to off-white
SMILES

OC(C=C1)=CC=C1C[C@@H]2C3=CC(OC)=C(OC)C=C3CCN2C
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
- Phenols
- Monophenols
Initial Source
- Plants
- other families
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1909 mL

15.9546 mL

31.9091 mL

5 mM

0.6382 mL

3.1909 mL

6.3818 mL

10 mM

0.3191 mL

1.5955 mL

3.1909 mL

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.

Molaritätsrechner

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

Mass

Konzentration

Volumen

Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Weng TC, et al. Inhibitory effects of armepavine against hepatic fibrosis in rats. J Biomed Sci. 2009;16(1):78. Published 2009 Sep 2. [Content Brief]

[2]. Jow GM, et al. Armepavine oxalate induces cell death on CCRF-CEM leukemia cell line through an apoptotic pathway. Life Sci. 2004;75(5):549-557. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Alle AP-1 Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Alle JNK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs