Dihydroberberine
Based on 1 Customer Validation
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy.
For research use only. We do not sell to patients.
- Purity: 99.30%
- CAS No.: 483-15-8
- Formula: C20H19NO4
- Molecular Weight:337.37
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Storage:
4°C, sealed storage, away from moisture and light
* The compound is unstable in solutions, freshly prepared is recommended.
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HSP90 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | CC50 |
155 μM
Compound: 10
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Cytotoxicity against MRC5 cells
Cytotoxicity against MRC5 cells
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[PMID: 17239594] |
| MRC5 | IC50 |
93 μM
Compound: 10
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Antiviral activity against HCMV in MRC5 cells by plaque reduction assay
Antiviral activity against HCMV in MRC5 cells by plaque reduction assay
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[PMID: 17239594] |
Dihydroberberine has a synergistic effect with sunitinib, and when mixed together, it exhibits anti-cancer effects in human non-small cell lung cancer cell lines (NSCLC), A549, NCI-H460 and NCI-H1299 cells. Dihydroberberine (25 μM; 48 h) inhibits NCI-H460 cell proliferation and colony formation[2].
NCI-H460 cells were treated with a mixture (DCS) of Dihydroberberine (25 μM) and Sunitinib (2 μM) to arrest the cell cycle in the G1 phase. DCS regulates JNK/p38 MAPK signaling and plays a role in inducing apoptosis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 483-15-8
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Appearance Solid
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Molecular Weight 337.37
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Formula C20H19NO4
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Color Light yellow to yellow
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SMILES
COC1=CC=C(C=C23)C(CN2CCC(C3=C4)=CC5=C4OCO5)=C1OC
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : 20 mg/mL (59.28 mM; ultrasonic and warming and heat to 70°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.93 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (14.82 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Yu D, et al. Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells. PLoS One. 2017 Aug 1;12(8):e0181823. [Content Brief]
[2]. Li C, et al. Dihydroberberine, an isoquinoline alkaloid, exhibits protective effect against dextran sulfate sodium-induced ulcerative colitis in mice. Phytomedicine. 2021 Sep;90:153631. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL |
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