Art. -Nr.: HY-N0671

Rhapontin

(Synonyms: Rhaponiticin)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Rhapontin (Rhaponiticin) is an orally aactive SIRT1 agonist and AMPK activator with anti-inflammatory and anti-fibrotic activities. Rhapontin inhibits NLRP3 inflammasome activation by activating SIRT1 and inhibits TGF-β/Smad signaling via the AMPK pathway. Rhapontin reduces intestinal and lung inflammation, inhibits fibroblast differentiation and extracellular matrix deposition, and enhances tight junction protein expression to repair epithelial barriers. Rhapontin can be used in the study of inflammatory bowel diseases (such as ulcerative colitis) and pulmonary fibrosis.

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Reinheit: 99.73%
CAS. Nr.: 155-58-8
Formel: C₂₁H₂₄O₉
Molecular Weight:420.41

Speicherung:

4°C, protect from light

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

Rhapontin Chemical Structure

CAS. Nr.: 155-58-8

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

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HCCLM3	IC₅₀	>100 μM Compound: 28	Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 34931827]
HepG2	IC₅₀	>100 μM Compound: 28	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 48 hrs by MTT assay	[PMID: 34931827]
KB	IC₅₀	34 nM Compound: RHA	Antitumor activity against FR-positive human KB cells assessed as decrease in cell viability measured after 48 hrs by MTT proliferation assay Antitumor activity against FR-positive human KB cells assessed as decrease in cell viability measured after 48 hrs by MTT proliferation assay	[PMID: 23177726]

In Vitro

Rhapontin (0.4-20 μM; 24 h) inhibits NLRP3 inflammasome activation, reduces IL-1β secretion, and reverses the activation of NF-κB and MAPK signaling pathways by upregulating SIRT1 expression in LPS-stimulated THP-1 macrophages^[1].
Rhapontin (0.4-10 μM; 24 h) inhibits NLRP3 inflammasome activation, reduces IL-1β secretion, and reverses the activation of NF-κB and MAPK signaling pathways by upregulating SIRT1 expression in LPS-stimulated THP-1 macrophages^[1].
Rhapontin (5-10 μM; 24 h) increases the expression of tight junction proteins ZO-1 and occludin, reduces the Bcl-2/Bax apoptotic protein ratio, and restores epithelial barrier function in NCM460 colon epithelial cells stimulated with TNF-α (10 ng/mL; 6 h)^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human intestinal colonic epithelial cells NCM460
Concentration:

0.4 µM, 2 µM, 10 µM
Incubation Time:

24 h
Result:

Significantly reduced the protein levels of NLRP3, cleaved caspase-1, and pro-inflammatory cytokines (IL-1β, TNF-α), while upregulating SIRT1 expression.
Inhibited phosphorylation of NF-κB p65 and MAPKs (ERK, JNK, p38) compared to the LPS-stimulated control group.

In Vivo

Rhapontin (100 mg/kg; gavage; once a day; 8 days) significantly reduces colon pathological damage in the DSS (HY-116282C)-induced acute colitis model in mice, inhibits inflammatory cell infiltration, MPO activity and NLRP3 inflammasome activation, and upregulates tight junction proteins ZO-1 and occludin to repair the epithelial barrier^[1].
Rhapontin (25-100 mg/kg; gavage; once a day; 14 days) significantly reduces lung tissue collagen deposition, inhibits TGF-β/Smad signaling pathway, activates AMPK and downregulates Lox2 and HIF-1α expression, and improves lung function^[2] in the Bleomycin (HY-108345)-induced pulmonary fibrosis model in mice^[1].

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

Animal Model:

C57BL/6 female mice (18-22 g, 6-8 weeks old), DSS-induced acute colitis model^[1]
Dosage:

100 mg/kg
Administration:

Gavage, once daily for 8 days (days 1-8 post-DSS induction).
Result:

Reduced disease activity index (DAI) score by 35% compared to the DSS group, with significant improvements in body weight loss, diarrhea, and hematochezia.
Histological analysis showed decreased inflammatory cell infiltration (lamina propria and submucosa), reduced crypt damage, and restored colon length.
MPO activity, a marker of neutrophil infiltration, was reduced by 42%.
Western blot showed decreased NLRP3, cleaved caspase-1, and TGF-β1 protein levels, while ZO-1 and occludin expressions were increased by 58% and 45%, respectively.

Animal Model:

C57BL/6 male mice (20-22 g, 6-8 weeks old) with Bleomycin (HY-108345)-induced pulmonary fibrosis model^[2]
Dosage:

25, 50, 100 mg/kg; Prednisone (6.5 mg/kg, positive control).
Administration:

Gavage, once daily for 14 days (days 7-21 post-bleomycin instillation).
Result:

At 100 mg/kg, reduced pulmonary index (lung weight/body weight) by 28% compared to the model group, with decreased collagen deposition.
Reduced TGF-β1, α-SMA, and Lox2 protein expressions by 41%, 37%, and 53%, respectively, while AMPK phosphorylation (p-AMPK/AMPK ratio) was increased by 62%.
ELISA showed decreased BALF levels of IL-1β.

Chemical Information

CAS. Nr. 155-58-8
Appearance Solid
Molecular Weight 420.41
Formel C₂₁H₂₄O₉
Color Off-white to yellow
SMILES

O[C@H]([C@@H](O)[C@@H]1O)[C@@H](O[C@@H]1CO)OC2=CC(/C=C/C3=CC(O)=C(OC)C=C3)=CC(O)=C2
Synonyms

Rhaponiticin
Structure Classification
- Phenols
- Polyphenols
- Stilbenes
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

Redox Biol

Gaylussacin, a stilbene glycoside, inhibits chronic obstructive pulmonary disease in mice. [Abstract]

2025 Jun 26:85:103744. PMID: 40614364
Biomed Res Int

Anti-influenza A Virus Effects and Mechanisms of Emodin and Its Analogs via Regulating PPAR α/ γ-AMPK-SIRT1 Pathway and Fatty Acid Metabolism. [Abstract]

2021 Sep 9;2021:9066938. PMID: 34540999

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (594.66 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

2.3786 mL

11.8932 mL

23.7863 mL

5 mM

0.4757 mL

2.3786 mL

4.7573 mL

10 mM

0.2379 mL

1.1893 mL

2.3786 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: ≥ 2.08 mg/mL (4.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (279 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 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]. Wei W, et al. Rhapontin ameliorates colonic epithelial dysfunction in experimental colitis through SIRT1 signaling. Int Immunopharmacol. 2017 Jan;42:185-194. [Content Brief]

[2]. Tao L, et al. Protective role of rhapontin in experimental pulmonary fibrosis in vitro and in vivo. Int Immunopharmacol. 2017 Jun;47:38-46. [Content Brief]

[3]. Hibasami H, et al. Induction of apoptosis by rhapontin having stilbene moiety, a component of rhubarb (Rheum officinale Baillon) in human stomach cancer KATO III cells. Oncol Rep. 2007 Aug;18(2):347-51. [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	2.3786 mL	11.8932 mL	23.7863 mL	59.4658 mL
	5 mM	0.4757 mL	2.3786 mL	4.7573 mL	11.8932 mL
	10 mM	0.2379 mL	1.1893 mL	2.3786 mL	5.9466 mL
	15 mM	0.1586 mL	0.7929 mL	1.5858 mL	3.9644 mL
	20 mM	0.1189 mL	0.5947 mL	1.1893 mL	2.9733 mL
	25 mM	0.0951 mL	0.4757 mL	0.9515 mL	2.3786 mL
	30 mM	0.0793 mL	0.3964 mL	0.7929 mL	1.9822 mL
	40 mM	0.0595 mL	0.2973 mL	0.5947 mL	1.4866 mL
	50 mM	0.0476 mL	0.2379 mL	0.4757 mL	1.1893 mL
	60 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9911 mL
	80 mM	0.0297 mL	0.1487 mL	0.2973 mL	0.7433 mL
	100 mM	0.0238 mL	0.1189 mL	0.2379 mL	0.5947 mL

Keywords

Rhapontin

2 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Rhapontin

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rhapontin Related Classifications

Art. -Nr.: HY-N0671