[CAS NO. 633-65-8]  Berberinechloride

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PRODUCTS SPECIFICATIONS [633-65-8]

Catalog
HY-18258
Brand
MCE
CAS
633-65-8

DESCRIPTION [633-65-8]

Overview

MDLMFCD00011939
Molecular Weight371.81
Molecular FormulaC20H18ClNO4
SMILESCOC1=C(OC)C2=C[N+]3=C(C(C(CC3)=C4)=CC5=C4OCO5)C=C2C=C1.[Cl-]

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


Summary

Berberine chloride is an alkaloid that acts as an antibiotic . Berberine chloride induces reactive oxygen species ( ROS ) generation and inhibits DNA topoisomerase . Antineoplastic properties [1] .


IC50 & Target

ROS [1]
DNA topoisomerase [1]


In Vitro

Berberine (1.25-160 μM; 72 hours) has potential inhibitory effects on the proliferation of four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29 [1] .
Berberine (1.25-160 μM; 24-72 hours) induces a time- and dose-dependent inhibition of LoVo cell growth [1] .
LoVo cells are exposure to Berberine (10-80 μM) for 24 h. Cell cycle analysis of 40 μM Berberine-treated LoVo cells by flow cytometry shows accumulation of cells in the G2/M phase [1] .
Berberine (10-80 μM) suppresses cyclin B1, cdc2 and cdc25c protein expression after 24 h, especially at the dose of 80.0 μM [1] .

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

Cell Proliferation Assay [1]

Cell Line: Four colorectal carcinoma cell lines LoVo, HCT116, SW480, and HT-29
Concentration: 1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM
Incubation Time: 72 hours
Result: Inhibited the proliferation of four cell lines. The IC 50 ranged from 40.8±4.1 μM (LoVo) to 98.6±2.9 μM (HCT116).

Cell Proliferation Assay [1]

Cell Line: Colorectal carcinoma cell lines LoVo
Concentration: 1.25, 2.5, 5, 10, 20, 40, 80, and 160 μM
Incubation Time: 24, 48, 72 hours
Result: Induced a time- and dose-dependent inhibition of cell growth. By 72 h, 160.0 μM induced 71.1±1.9 % growth inhibitions in LoVo cells.

Cell Cycle Analysis [1]

Cell Line: LoVo cells
Concentration: 0, 10, 20, 40, or 80 μM
Incubation Time: 24 hours
Result: Exposure to 40.0 μM induced G2/M-phase cell cycle arrest, an increase in the G2/M-phase population and a progressive decline in the G1 population.

Western Blot Analysis [1]

Cell Line: LoVo cells
Concentration: 10, 20, 40, or 80 μM
Incubation Time: 24 hours
Result: Suppressed cyclin B1, cdc2 and cdc25c protein expression.

In Vivo

Berberine (10, 30, or 50 mg/kg/day; gastrointestinal gavage; for 10 consecutive days) inhibits the growth of human colorectal adenocarcinoma in vivo. Berberine at doses of 30 and 50 mg/kg/day taken by gastrointestinal gavage shows inhibitory rates of 33.1% and 45.3% on the human colorectal adenocarcinoma xenograft growth in nude mice [1] .

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

Animal Model: 5-week-old BALB/c nu/nu mice with human colorectal adenocarcinoma LoVo xenografts [1]
Dosage: 10, 30, or 50 mg/kg/day
Administration: Gastrointestinal gavage; for 10 consecutive days
Result: Showed inhibitory rates of 33.1 % and 45.3 % at doses of 30 and 50 mg/kg/day.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT03609892 Xijing Hospital of Digestive Diseases
Gastric Ulcer|Chronic Gastritis|Gastric Cancer|Helicobacter Pylori Infection|Gastritis
August 1, 2018 Phase 4
NCT02226185 Shanghai Jiao Tong University School of Medicine
Colorectal Adenoma
November 2014 Phase 2|Phase 3
NCT03378934 Peking Union Medical College Hospital
Coronary Artery Disease|Percutaneous Coronary Intervention
September 26, 2018 Phase 4

Appearance

Solid



Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture

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


Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL ( 33.62 mM ; Need ultrasonic)

H 2 O : < 0.1 mg/mL (ultrasonic) (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6895 mL 13.4477 mL 26.8955 mL
5 mM 0.5379 mL 2.6895 mL 5.3791 mL
10 mM 0.2690 mL 1.3448 mL 2.6895 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 0.5% CMC-Na /saline water

    Solubility: 11 mg/mL (29.59 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one: PBS

    Solubility: 10 mg/mL (26.90 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.25 mg/mL (3.36 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

Benzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium, 5,6-dihydro-9,10-dimethoxy-, chloride (1:1)
Berbinium, 7,8,13,13a-tetradehydro-9,10-dimethoxy-2,3-(methylenedioxy)-, chloride
Benzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium, 5,6-dihydro-9,10-dimethoxy-, chloride
Berberine, chloride
Berberine hydrochloride
Berberinium chloride
NSC 646666
NSC 163088
Berberine IR
16,17-Dimethoxy-5,7-dioxa-13λ5-azapentacyclo[11.8.0.0[2,10].0[4,8].0[15,20]]henicosa-1(21),2(10),3,8,13,15(20),16,18-octaen-13-ylium chloride