Art. -Nr.: HY-N2484

Methylnissolin

(Synonyms: Astrapterocarpan)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

Methylnissolin (Astrapterocarpan) is an osteoclast inhibitor with anti-inflammatory, neuroprotective and antioxidant activities. Methylnissolin downregulates the activation of the MAPK and PI3K/AKT pathways, inhibits the phosphorylation of MAPK1 and AKT1, and blocks PDGF-BB-induced phosphorylation of ERK1/2. Methylnissolin reduces the expression and secretion of proinflammatory mediators, decreases intracellular ROS levels, upregulates antioxidant enzymes, and downregulates osteoclastogenesis markers. Methylnissolin is applicable to research related to ischemic stroke, osteoporosis, cardiovascular diseases, skin aging, etc.

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Reinheit: 99.92%
CAS. Nr.: 73340-41-7
Formel: C₁₇H₁₆O₅
Molecular Weight:300.31

Speicherung:

4°C, protect from light

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

Methylnissolin Chemical Structure

CAS. Nr.: 73340-41-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PDGFR

10 μM (IC₅₀)

ERK1

ERK2

Alle PDGFR Isoform-spezifische Produkte anzeigen :

Alle ERK Isoform-spezifische Produkte anzeigen :

In Vitro

Methylnissolin (Astrapterocarpan) (0.5-50 μM; 24 h) shows no significant cytotoxicity to primary mouse microglia at concentrations up to 10 μM after 24 h of incubation^[1].
Methylnissolin (5-10 μM; 6 h/24 h) inhibits the pro-inflammatory response triggered by OGD/R in primary mouse microglia by reducing the expression and secretion of key pro-inflammatory mediators at concentrations of 5 and 10 μM^[1].
Methylnissolin (5-10 μM) modulates the PI3K/AKT and MAPK signaling pathways in OGD/R-treated primary mouse microglia, reducing phosphorylation of key pathway proteins at concentrations of 5 and 10 μM^[1].
Methylnissolin stably binds to purified MAPK1 and AKT1 proteins with high affinity, with binding energies of -7.302 kcal/mol and -7.734 kcal/mol, respectively^[2].
Methylnissolin (0-100 μM; 48-96 h) does not reduce the viability of BMMs^[2].
Methylnissolin (25-100 μM; 6 days) potently inhibits RANKL-induced osteoclast differentiation from BMMs in a dose- and time-dependent manner, with peak activity during days 3-6 of the 6-day differentiation period^[2].
Methylnissolin (50-100 μM; 48 h) disrupts cytoskeletal organization of RANKL-stimulated BMM-derived osteoclasts in a concentration-dependent manner, reducing F-actin ring formation at 50 and 100 μM^[2].
Methylnissolin (50-100 μM; 48 h) reduces intracellular ROS levels in RANKL-stimulated BMMs in a concentration-dependent manner, with significant effects observed at 50 and 100 μM after 48 h^[2].
Methylnissolin (50-100 μM) activates the Nrf2-mediated antioxidant defense pathway in RANKL-stimulated BMMs, increasing the expression of Nrf2, CAT, and HO-1 proteins at 50 and 100 μM^[2].
Methylnissolin (100 μM; days 1, 3, 5 of differentiation) suppresses the expression of critical osteoclastogenic proteins in RANKL-stimulated BMMs, with reduced NFATc1 at days 3 and 5, and reduced c-Fos at days 1 and 3 of differentiation^[2].
Methylnissolin (100 μM; pre-treatment, 10-60 min post-RANKL stimulation) inhibits RANKL-induced activation of the MAPK and AKT signaling pathways in BMMs, reducing ERK phosphorylation at 10 and 20 min, and AKT phosphorylation at 20 min post-stimulation^[2].
Methylnissolin (1-50 μM; 24 h) inhibits PDGF-BB-induced ERK1/2 phosphorylation in A10 vascular smooth muscle cells in vitro in a concentration-dependent manner with an IC₅₀ of 10 μM after 24 h of pre-incubation, but does not affect PDGF-BB-induced phosphorylation of p38 MAPK or Akt^[3].
Methylnissolin (25-100 μM; 24 h) is non-cytotoxic to human dermal fibroblasts^[4].
Methylnissolin (25-100 μM; 1 h pre-incubation) dose-dependently inhibits TNF-α-induced intracellular ROS generation in human dermal fibroblasts, with significant suppression observed^[4].
Methylnissolin (25-100 μM; 1 h pre-incubation, 24 h TNF-α exposure) dose-dependently inhibits TNF-α-induced MMP-1 secretion in human dermal fibroblasts, with significant suppression observed, but does not enhance COLIA1 secretion^[4].
Methylnissolin (100 μM; 1 h pre-incubation, 24 h TNF-α exposure) inhibits TNF-α-induced MMP-1 mRNA expression in human dermal fibroblasts^[4].
Methylnissolin demonstrates favorable oral drug-likeness properties, including high gastrointestinal absorption, but interacts with multiple CYP450 enzymes, and has higher skin permeability than its glucoside analog^[4].

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

Cell Differentiation Assay^[2]

Cell Line:

RANKL-stimulated bone marrow-derived macrophages (BMMs)
Concentration:

25-100 μM; 100 μM (days 1-2, days 3-4, days 5-6, or days 1-6 of differentiation)
Incubation Time:

6 days; variable time windows during 6-day differentiation period
Result:

Caused dose-dependent suppression of multinucleated TRAP-positive osteoclast formation.
Showed peak inhibitory activity when added between days 3 and 6 of culture.

Real Time qPCR^[2]

Cell Line:

RANKL-stimulated bone marrow-derived macrophages (BMMs)
Concentration:

50-100 μM
Incubation Time:

6 days
Result:

Coordinatedly downregulated the expression of osteoclastogenic genes including Nfatc1, Fos, Ctsk, Mmp9, Atp6v0d2, and Acp5.

Western Blot Analysis^[2]

Cell Line:

RANKL-stimulated bone marrow-derived macrophages (BMMs)
Concentration:

100 μM
Incubation Time:

Analyzed at days 1, 3, and 5 of differentiation
Result:

Suppressed NFATc1 protein expression during days 3 and 5 of differentiation, and reduced c-Fos protein expression at days 1 and 3.

Western Blot Analysis^[2]

Cell Line:

RANKL-stimulated bone marrow-derived macrophages (BMMs)
Concentration:

100 μM
Incubation Time:

Pre-treatment, analyzed at 10, 20, 30, 60 min post-RANKL stimulation
Result:

Significantly suppressed ERK phosphorylation at 10 and 20 min following RANKL stimulation, and reduced AKT phosphorylation at the 20-min activation window.

Cell Cytotoxicity Assay^[3]

Cell Line:

A10 vascular smooth muscle cells
Concentration:

1-50 μM
Incubation Time:

48 h
Result:

Showed LDH release percentages of 12.9%, 13.2%, 12.3%, 12.5%, 12.1% at concentrations 1, 5, 10, 25, 50 μM respectively, which were not significantly different from the control group's 12.1% LDH release.

Cell Proliferation Assay^[3]

Cell Line:

PDGF-BB-stimulated A10 vascular smooth muscle cells
Concentration:

1-50 μM
Incubation Time:

48 h (co-incubated with PDGF-BB)
Result:

Inhibited PDGF-BB-stimulated cell proliferation in a concentration-dependent manner, with significant inhibition at 1 μM.
Reached an IC₅₀ value of 10 μM for the inhibitory effect.

Western Blot Analysis^[3]

Cell Line:

PDGF-BB-stimulated A10 vascular smooth muscle cells
Concentration:

1-50 μM
Incubation Time:

24 h (pre-incubation); 20 min (PDGF-BB stimulation)
Result:

Did not reduce PDGF-BB-induced tyrosine phosphorylation of the PDGF-β-receptor, as measured by densitometric analysis of immunoblot bands.\nInhibited PDGF-BB-induced phosphorylation of ERK1/2 in a concentration-dependent manner, with significant inhibition at 5 μM and an IC₅₀ value of 10 μM.
Did not inhibit PDGF-BB-induced phosphorylation of p38 MAPK or Akt at any tested concentration.

ELISA Assay^[4]

Cell Line:

TNF-α-stimulated human dermal fibroblasts (HDFs)
Concentration:

25, 50, 100 μM
Incubation Time:

1 h (pre-incubation) + 24 h (TNF-α exposure)
Result:

Reduced TNF-α-induced 2.71-fold MMP-1 secretion to 2.08-fold (25 μM), 1.88-fold (50 μM), and 0.86-fold (100 μM) relative to the control group.
Did not increase COLIA1 secretion in TNF-α-stimulated HDFs.

Real Time qPCR^[4]

Cell Line:

TNF-α-stimulated human dermal fibroblasts (HDFs)
Concentration:

100 μM
Incubation Time:

1 h (pre-incubation) + 24 h (TNF-α exposure)
Result:

Reduced TNF-α-induced MMP-1 mRNA expression to 1.1-fold relative to the control group.

In Vivo

Methylnissolin (Astrapterocarpan) (10-20 mg/kg/day) reduces ischemic brain injury, attenuates microglia-mediated neuroinflammation, and improves neurological function in tMCAO mice^[1].
Methylnissolin (10-20 mg/kg; 6 continuous weeks) dose-dependently prevents ovariectomy-induced postmenopausal osteoporosis in female C57BL/6 mice by improving trabecular bone parameters and reducing osteoclast activity, with no detected toxicity^[2].

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

Animal Model:

C57BL/6 (female, 8 weeks old, 20±2 g, bilateral ovariectomy-induced)^[2]
Dosage:

10 mg/kg; 20 mg/kg
Administration:

6 continuous weeks
Result:

Restored trabecular bone volume fraction (BV/TV).
Increased trabecular number (Tb.N).
Increased trabecular thickness (Tb.Th).
Decreased trabecular separation (Tb.Sp).
Significantly restored bone surface/tissue surface (BS/TS) in femoral trabecular bone.
Reduced the number of osteoclasts per bone surface (N.OC/BS) in femoral trabecular bone.
Elevated Nrf2 and HO-1 expression in trabecular bone.
Showed no detectable toxicity in cardiac, hepatic, splenic, pulmonary, or renal tissues.

Chemical Information

CAS. Nr. 73340-41-7
Appearance Solid
Molecular Weight 300.31
Formel C₁₇H₁₆O₅
Color White to off-white
SMILES

COC1=C2O[C@]3([H])[C@](COC4=CC(O)=CC=C34)([H])C2=CC=C1OC
Synonyms

Astrapterocarpan
Structure Classification
- Flavonoids
- Other Flavonoids
- Phenols
- Monophenols
Initial Source
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)

Publications (2)

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Journal Impact Factor

Int Immunopharmacol

Dual suppression of AKT/MAPK signaling and activation of Nrf2 by methylnissolin attenuates osteoclastogenesis and prevents postmenopausal osteoporosis. [Abstract]

2025 Dec 2:169:115942. PMID: 41337836
J Cell Mol Med

Jinbei Decoction Attenuates LPS-Induced Acute Lung Injury via Suppression of TRAF6-Dependent Inflammatory Response in Macrophage. [Abstract]

2025 Nov;29(21):e70944. PMID: 41230791

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (166.49 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

3.3299 mL

16.6495 mL

33.2989 mL

5 mM

0.6660 mL

3.3299 mL

6.6598 mL

10 mM

0.3330 mL

1.6649 mL

3.3299 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 Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

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

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(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 (8.32 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 (8.32 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 (8.32 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals 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 (291 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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]. Wu J, et al. Methylnissolin mitigates microglia-mediated neuroinflammation and ischemic brain injury through PI3K/AKT and MAPK pathways. Eur J Pharmacol. 2026;1011:178431. [Content Brief]

[2]. Feng Y, et al. Dual suppression of AKT/MAPK signaling and activation of Nrf2 by methylnissolin attenuates osteoclastogenesis and prevents postmenopausal osteoporosis. Int Immunopharmacol. 2026;169:115942. [Content Brief]

[3]. Ohkawara S, et al. Astrapterocarpan isolated from Astragalus membranaceus inhibits proliferation of vascular smooth muscle cells. Eur J Pharmacol. 2005;525(1-3):41-47. [Content Brief]

[4]. Choi YJ, et al. Protective effects of methylnissolin and methylnissolin-3-O-β-d-glucopyranoside on TNF-α-induced inflammation in human dermal fibroblasts. Toxicol In Vitro. 2025;104:106005. [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	3.3299 mL	16.6495 mL	33.2989 mL	83.2473 mL
	5 mM	0.6660 mL	3.3299 mL	6.6598 mL	16.6495 mL
	10 mM	0.3330 mL	1.6649 mL	3.3299 mL	8.3247 mL
	15 mM	0.2220 mL	1.1100 mL	2.2199 mL	5.5498 mL
	20 mM	0.1665 mL	0.8325 mL	1.6649 mL	4.1624 mL
	25 mM	0.1332 mL	0.6660 mL	1.3320 mL	3.3299 mL
	30 mM	0.1110 mL	0.5550 mL	1.1100 mL	2.7749 mL
	40 mM	0.0832 mL	0.4162 mL	0.8325 mL	2.0812 mL
	50 mM	0.0666 mL	0.3330 mL	0.6660 mL	1.6649 mL
	60 mM	0.0555 mL	0.2775 mL	0.5550 mL	1.3875 mL
	80 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0406 mL
	100 mM	0.0333 mL	0.1665 mL	0.3330 mL	0.8325 mL

Keywords

Methylnissolin

2 Cited Publications

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Methylnissolin

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Publications Citing Use of MedChemExpress (MCE) Methylnissolin

Alle PDGFR Isoform-spezifische Produkte anzeigen

Alle ERK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Methylnissolin Related Classifications

HY-N2484 Related Classifications