2. Metabolic Enzyme/Protease Neuronal Signaling Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage PI3K/Akt/mTOR Epigenetics
  3. Phosphatase Monoamine Oxidase PPAR mTOR AMPK
  4. Rubrofusarin gentiobioside

Rubrofusarin gentiobioside  (Synonyms: Rubrofusarin-6-β-gentiobioside)

Cat. No.: HY-N4177 Purity: 99.04%
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Rubrofusarin gentiobioside (Rrubrofusarin-6-β-gentiobioside) is an orally active weak inhibitor of PTP1B and MAO-A (IC50 >100 μM), and its glycosylation modification results in lower biological activity than its aglycone Rubrofusarin (HY-130307). Rubrofusarin gentiobioside promotes AMPK phosphorylation in an LKB1-independent manner and inhibits the mTOR signaling pathway, thereby downregulating the expressions of PPARγ, C/EBPα, as well as FAS, LPL and aP2. Rubrofusarin gentiobioside inhibits lipid accumulation, reduces body weight and epididymal white adipose tissue volume, improves fatty liver, and shows no cytotoxicity to hepatocytes. Rubrofusarin gentiobioside is widely used in obesity-related studies.

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

Rubrofusarin gentiobioside

Rubrofusarin gentiobioside Chemical Structure

CAS No. : 24577-90-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Rubrofusarin gentiobioside Related Antibodies

Top Publications Citing Use of Products

View All Monoamine Oxidase Isoform Specific Products:

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MAO-A MAO-B

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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mTOR mTORC1 mTORC2

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NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rubrofusarin gentiobioside (Rrubrofusarin-6-β-gentiobioside) is an orally active weak inhibitor of PTP1B and MAO-A (IC50 >100 μM), and its glycosylation modification results in lower biological activity than its aglycone Rubrofusarin (HY-130307). Rubrofusarin gentiobioside promotes AMPK phosphorylation in an LKB1-independent manner and inhibits the mTOR signaling pathway, thereby downregulating the expressions of PPARγ, C/EBPα, as well as FAS, LPL and aP2. Rubrofusarin gentiobioside inhibits lipid accumulation, reduces body weight and epididymal white adipose tissue volume, improves fatty liver, and shows no cytotoxicity to hepatocytes. Rubrofusarin gentiobioside is widely used in obesity-related studies[1][2].

IC50 & Target[1]

MAO-A

 

PPAR-γ

 

In Vitro

Rubrofusarin gentiobioside (200, 400 μM; 48 h) is non-cytotoxic to 3T3-L1 murine pre-adipocytes[1].
Rubrofusarin gentiobioside (50, 100, 200 μM) activates AMPKα in an LKB1-independent manner, suppresses mTOR phosphorylation, and does not regulate the PI3K/AKT pathway in differentiated 3T3-L1 murine pre-adipocytes at concentrations of 50, 100, and 200 μM[1].
Rubrofusarin gentiobioside (400 μM; 48 h) is non-cytotoxic to human adipose mesenchymal stem cells at concentrations up to 400 μM when incubated for 48 h[1].
Rubrofusarin gentiobioside (25-100 μM) is non-toxic to HepG2 human hepatocarcinoma cells at concentrations up to 100 μM[2].
Rubrofusarin gentiobioside has limited druglike properties per Lipinski’s rule and poor predicted ADME characteristics including low intestinal absorption and blood-brain barrier penetration[2].

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

Rubrofusarin gentiobioside Related Antibodies

Cell Viability Assay[1]

Cell Line: 3T3-L1 murine pre-adipocytes
Concentration: 0, 50, 100, 200, 400 μM
Incubation Time: 48 h
Result: Did not exert cytotoxicity at concentrations up to 200 μM.
Caused a statistically significant reduction in cell viability (p < 0.05) relative to the untreated control at 400 μM.

Cell Viability Assay[1]

Cell Line: human adipose mesenchymal stem cells (hAMSCs)
Concentration: 0, 50, 100, 200, 400 μM
Incubation Time: 48 h
Result: Did not exhibit cytotoxicity at any tested concentration up to 400 μM.
In Vivo

Rubrofusarin gentiobioside (50-100 mg/kg/day; p.o.; daily; 10 weeks) dose-dependently reduces weight gain, adipocyte size, hepatic steatosis, and dysregulated serum lipid levels in HFD-induced obese mice[1].

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

Animal Model: C57BL/6 J mice with Obesity (male, 4 weeks old, 16-18 g, HFD-induced obesity)[1]
Dosage: 50 mg/kg/day; 100 mg/kg/day
Administration: p.o.; daily; 10 weeks
Result: Reduced weight gain by 19.7% (50 mg/kg/day) and 30.9% (100 mg/kg/day) relative to HFD-only group.
Reduced epididymal white adipose tissue weight relative to HFD-only group.
Prevented liver weight increase relative to HFD-only group.
Decreased serum total cholesterol, LDL-cholesterol, free fatty acid, glucose, and leptin levels, and increased adiponectin levels relative to HFD-only group.
Reduced adipocyte size to 4079 μM2 (50 mg/kg/day) and 2813 μM2 (100 mg/kg/day) relative to 5944 μM2 in HFD-only group.
Reduced hepatic lipid accumulation relative to HFD-only group.
Decreased protein and mRNA expression of PPARγ and C/EBPα in epididymal white adipose tissue and liver relative to HFD-only group.
Increased phosphorylation of AMPK and decreased phosphorylation of mTOR in epididymal white adipose tissue and liver relative to HFD-only group.
Downregulated mRNA expression of FAS, LPL, and aP2 in epididymal white adipose tissue and liver relative to HFD-only group.
Molecular Weight

596.53

Formula

C27H32O15
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O[C@H]1[C@H](OC2=CC(OC)=CC3=C2C(O)=C4C(C=C(C)OC4=C3)=O)O[C@H](CO[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)CO)O)O)O)[C@@H](O)[C@@H]1O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (167.64 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 1.6764 mL 8.3818 mL 16.7636 mL
5 mM 0.3353 mL 1.6764 mL 3.3527 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 (sealed storage, away from moisture and 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)

Mass
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Concentration
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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)

V1

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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 (4.19 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 (4.19 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

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.
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 (sealed storage, away from moisture and 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
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 (sealed storage, away from moisture and 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 1.6764 mL 8.3818 mL 16.7636 mL 41.9090 mL
5 mM 0.3353 mL 1.6764 mL 3.3527 mL 8.3818 mL
10 mM 0.1676 mL 0.8382 mL 1.6764 mL 4.1909 mL
15 mM 0.1118 mL 0.5588 mL 1.1176 mL 2.7939 mL
20 mM 0.0838 mL 0.4191 mL 0.8382 mL 2.0955 mL
25 mM 0.0671 mL 0.3353 mL 0.6705 mL 1.6764 mL
30 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3970 mL
40 mM 0.0419 mL 0.2095 mL 0.4191 mL 1.0477 mL
50 mM 0.0335 mL 0.1676 mL 0.3353 mL 0.8382 mL
60 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6985 mL
80 mM 0.0210 mL 0.1048 mL 0.2095 mL 0.5239 mL
100 mM 0.0168 mL 0.0838 mL 0.1676 mL 0.4191 mL
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Rubrofusarin gentiobioside 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:

Rubrofusarin gentiobioside24577-90-0Rubrofusarin-6-β-gentiobiosidePhosphataseMonoamine OxidasePPARmTORAMPKMAOPeroxisome proliferator-activated receptorsMammalian target of RapamycinAMP-activated protein kinase3T3-L1 murine pre-adipocytesC/EBPαhMAO-Ahuman PTP1BPPARγLPLLKB1FASInhibitorinhibitorinhibit

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