Art. -Nr.: HY-N5027

Oxyberberine

(Synonyms: Oxyberberin; Berlambine; 8-Oxoberberine)

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

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.

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Reinheit: 99.78%
CAS. Nr.: 549-21-3
Formel: C₂₀H₁₇NO₅
Molecular Weight:351.35

Speicherung:

4°C, protect from light

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

Oxyberberine Chemical Structure

CAS. Nr.: 549-21-3

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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
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 549-21-3
Appearance Solid
Molecular Weight 351.35
Formel C₂₀H₁₇NO₅
Color Light yellow to yellow
SMILES

O=C(C1=C(OC)C(OC)=CC=C1C=C23)N2CCC(C3=C4)=CC5=C4OCO5
Synonyms

Oxyberberin; Berlambine; 8-Oxoberberine
Structure Classification
- Alkaloids
- Isoquinoline Alkaloids
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

Hepatol Commun

Oxyberberine sensitizes liver cancer cells to sorafenib via inhibiting NOTCH1-USP7-c-Myc pathway. [Abstract]

2024 Mar 29;8(4):e0405. PMID: 38573832
SSRN

2023 Jan 27.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 16.67 mg/mL (47.45 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

2.8462 mL

14.2308 mL

28.4616 mL

5 mM

0.5692 mL

2.8462 mL

5.6923 mL

10 mM

0.2846 mL

1.4231 mL

2.8462 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: ≥ 1.67 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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% Corn Oil

Solubility: ≥ 1.67 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 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 (16.7 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 (283 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]. Dou Y, et al. In vitro and in vivo hypoglycemia effect of oxyberberine, a novel HO-1 agonist: A renewed evidence linking HO-1 to diabetes mellitus. Phytomedicine. 2022 Jul;101:154135. [Content Brief]

[2]. Li C, et al. Oxyberberine ameliorates TNBS-induced colitis in rats through suppressing inflammation and oxidative stress via Keap1/Nrf2/NF-κB signaling pathways. Phytomedicine. 2023 Jul 25;116:154899. [Content Brief]

[3]. Tentu PM, et al. Oxyberberine an oxoderivative of berberine confers neuroprotective effects in controlled-cortical impact mouse model of traumatic brain injury. Int J Neurosci. 2025 Jan;135(1):80-95. [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	2.8462 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

Keywords

Oxyberberine

2 Cited Publications

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Oxyberberine

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Publications Citing Use of MedChemExpress (MCE) Oxyberberine

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Oxyberberine Related Classifications

HY-N5027 Related Classifications