2. Natural Products
  3. Disease Research Fields Plants Stilbenes
  4. Rutaceae Infection
  5. Phellodendron amurense Rupr.
  6. Oxyberberine

Oxyberberine  (Synonyms: Oxyberberin; Berlambine; 8-Oxoberberine)

Cat. No.: HY-N5027 Purity: 99.85%
SDS
COA
Handling Instructions Technical Support

Oxyberberine (Oxyberberin; Berlambine) is an orally effective heme oxygenase HO-1 agonist that can activate antioxidant mechanisms by regulating the PI3K/Akt/AMPK signaling pathway. Oxyberberine induces HO-1 expression, increases SOD and GSH-Px activity, inhibits NF-κB-mediated inflammatory responses, and improves insulin sensitivity and glucose metabolism. Oxyberberine has anti-diabetic, neuroprotective, anti-inflammatory and antioxidant effects, and can be used to study type 2 diabetes, traumatic brain injury (TBI) and inflammatory bowel disease.

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

Oxyberberine Chemical Structure

Oxyberberine Chemical Structure

CAS No. : 549-21-3

Size Price Stock Quantity
5 mg In-stock
10 mg In-stock
20 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Oxyberberine Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Oxyberberine (Oxyberberin; Berlambine) is an orally effective heme oxygenase HO-1 agonist that can activate antioxidant mechanisms by regulating the PI3K/Akt/AMPK signaling pathway. Oxyberberine induces HO-1 expression, increases SOD and GSH-Px activity, inhibits NF-κB-mediated inflammatory responses, and improves insulin sensitivity and glucose metabolism. Oxyberberine has anti-diabetic, neuroprotective, anti-inflammatory and antioxidant effects, and can be used to study type 2 diabetes, traumatic brain injury (TBI) and inflammatory bowel disease[1][2][3].

Cellular Effect
Cell Line Type Value Description References
PC-12 CC50
137 μM
Compound: 2
Cytotoxicity against rat PC12 cells assessed as reduction in cell viability incubated for 24 hrs by WST-8 assay
Cytotoxicity against rat PC12 cells assessed as reduction in cell viability incubated for 24 hrs by WST-8 assay
[PMID: 33611188]
In Vitro

Oxyberberine (5-20 μM; 24-48 h) promotes glucose-stimulated insulin secretion in INS-1 cells, reduces intracellular reactive oxygen species (ROS) and malondialdehyde (MDA) levels, and increases superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) activities[1].
Oxyberberine (10-40 μM; 24 h) enhances glucose consumption, upregulates phosphorylated Akt (p-Akt) and GSK-3β (p-GSK-3β) expressions, and downregulates glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) levels in insulin-resistant HepG2 cells[1].

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

Oxyberberine Related Antibodies

Western Blot Analysis[1]

Cell Line: INS-1 cells
Concentration: 5, 10, 20 μM
Incubation Time: 48 h
Result: Dose-dependently increased insulin secretion in high-glucose (25 mM) stimulated INS-1 cells, reduced oxidative stress markers (NO, MDA) and increased antioxidant enzymes (SOD, GSH-Px).
Co-treatment with HO-1 inhibitor ZnPP reversed these effects, indicating dependency on HO-1 activation.

Western Blot Analysis[1]

Cell Line: Insulin-resistant HepG2 cells
Concentration: 10, 20, 40 μM
Incubation Time: 24 h
Result: Significantly increased glucose consumption in insulin-resistant HepG2 cells.
Western blot analysis showed upregulation of p-Akt, p-GSK-3β and downregulation of G6Pase, PEPCK, with the most pronounced effects at 40 μM.
Co-administration of ZnPP attenuated these changes, suggesting involvement of HO-1 signaling.
In Vivo

Oxyberberine (50, 100 mg/kg; gavage; once a day; 6 weeks) significantly reduces fasting blood glucose, glycosylated serum protein (GSP) and blood lipid levels in the HFD/STZ-induced rat type 2 diabetes model, and improves insulin resistance and pancreatic tissue pathological damage[1].
Oxyberberine can significantly alleviate DSS-induced ulcerative colitis in mice, which may be related to the inhibition of TLR4/Myd88/NF-κB pathway excitation and regulation of intestinal flora. LD50 >5000 mg/kg. Oxyberberine (12.5-50 mg/kg; intraperitoneal injection; once daily; 21 days) significantly improves colon tissue pathological damage in the TNBS-induced rat colitis model, reduces the proinflammatory markers TNF-α, IL-2, IL-8 and IL-22, and increases the levels of IL-4 and IL-13[2].
Oxyberberine (25, 50 mg/kg; intraperitoneal injection; once daily; 21 days) alleviates neurological deficits, improves anxiety-like behaviors and cognitive impairment in the traumatic brain injury (TBI) model of male C57BL/6 mice, and inhibits the HMGB1-mediated TLR4/NF-κB inflammatory pathway in brain tissue[3].

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

Animal Model: Male Sprague-Dawley rats (220-240 g, 7-week-old) with high-fat diet/streptozotocin (HFD/STZ)-induced type 2 diabetes[1]
Dosage: 50 mg/kg, 100 mg/kg (saline)
Administration: Oral gavage, once daily, for 6 weeks
Result: Significantly decreased fasting blood glucose (FBG), triglyceride (TG), total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), and glycosylated serum protein (GSP), while increasing high-density lipoprotein cholesterol (HDL-C).
Improved insulin sensitivity (reduced HOMA-IR), pancreatic antioxidant capacity (increased SOD, GSH-Px), and attenuated islet cell apoptosis and inflammatory cytokine levels (TNF-α, IL-6).
Co-treatment with HO-1 inhibitor ZnPP reversed these effects.
Animal Model: Male C57BL/6 mice (6-8-week-old) with traumatic brain injury (TBI)-induced traumatic brain injury[3]
Dosage: 25 mg/kg, 50 mg/kg (saline)
Administration: Intraperitoneal injection, once daily, for 21 days
Result: Significantly reduced neurological severity scores (NSS) and improved motor coordination in rotarod tests.
Decreased anxiety-like behavior in elevated zero maze (EZM) and improved cognitive performance in novel object recognition task (NORT).
Western blot showed reduced expression of HMGB1, TLR4, and NF-κB in ipsilateral cortex, with the highest efficacy at 50 mg/kg.
Molecular Weight

351.35

Formula

C20H17NO5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(OC)C(OC)=CC=C1C=C23)N2CCC(C3=C4)=CC5=C4OCO5
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 : 16.67 mg/mL (47.45 mM; ultrasonic and warming and heat to 60°C; 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 2.8462 mL 14.2308 mL 28.4616 mL
5 mM 0.5692 mL 2.8462 mL 5.6923 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 (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: 99.85%

SDS (393 KB)

COA (251 KB) HNMR (187 KB) LCMS (112 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 2.8462 mL 14.2308 mL 28.4616 mL 71.1541 mL
5 mM 0.5692 mL 2.8462 mL 5.6923 mL 14.2308 mL
10 mM 0.2846 mL 1.4231 mL 2.8462 mL 7.1154 mL
15 mM 0.1897 mL 0.9487 mL 1.8974 mL 4.7436 mL
20 mM 0.1423 mL 0.7115 mL 1.4231 mL 3.5577 mL
25 mM 0.1138 mL 0.5692 mL 1.1385 mL 2.8462 mL
30 mM 0.0949 mL 0.4744 mL 0.9487 mL 2.3718 mL
40 mM 0.0712 mL 0.3558 mL 0.7115 mL 1.7789 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Oxyberberine 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:

Oxyberberine549-21-3Oxyberberin Berlambine 8-OxoberberineOthersInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Oxyberberine
Cat. No.:
HY-N5027
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.