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Purity: ≥98%
Epiberberine Chloride, an alkaloid, is a natural anticancer agent isolated from Coptis chinensis with the potential for the treatment of diabetic disease., it acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. It stabilizes telomeric G4s and inhibits telomerase, specifically recognizing the hybrid-2 telomeric G4 predominant in physiologically relevant K+ solution and converts other telomeric G4 forms to hybrid-2. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO- scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease. Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways.
| ln Vitro |
In 3T3-L1 adipocytes, epiberberine (0, 12.5, 25 or 50 μM) suppresses cellular triglyceride accumulation in a dose-dependent manner, with an IC50 of 52.8 μM [2]. During the initial stages of 3T3-L1 adipocyte development, epiberberine (12.5-50 μM) suppresses the Raf/MEK1/ERK1/2 and AMPKα/Akt pathways. The concentration-dependent inhibition of glucose absorption in HepG2 cells is caused by epiberberine (0.2, 1, 5 μg/mL) [3].
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| ln Vivo |
In KK-Ay mice, oral administration of epiberberine (225 mg/kg) for 40 days results in decreased body weight, food consumption, water intake, and urine output [3].
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| References |
[1]. Jung HA, et al. Anti-Alzheimer and antioxidant activities of Coptidis Rhizoma alkaloids. Biol Pharm Bull. 2009 Aug;32(8):1433-8.
[2]. Choi JS, et al. Anti-adipogenic effect of epiberberine is mediated by regulation of the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways. Arch Pharm Res. 2015 Dec;38(12):2153-62. [3]. Ma H, et al. Antihyperglycemia and Antihyperlipidemia Effect of Protoberberine Alkaloids From Rhizoma Coptidis in HepG2 Cell and Diabetic KK-Ay Mice. Drug Dev Res. 2016 Jun;77(4):163-70 |
| Molecular Formula |
C20H18CLNO4
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|---|---|
| Molecular Weight |
371.814224720001
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| CAS # |
889665-86-5
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| Related CAS # |
Epiberberine;6873-09-2
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| SMILES |
COC1=CC2=C(C3=[N+](CC2)C=C4C(OCO5)=C5C=CC4=C3)C=C1OC.[Cl-]
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| InChi Key |
DGRBIBRPLDAHJH-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C20H18NO4.ClH/c1-22-18-8-13-5-6-21-10-15-12(3-4-17-20(15)25-11-24-17)7-16(21)14(13)9-19(18)23-2;/h3-4,7-10H,5-6,11H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
8,9-Dimethoxy-11,12-dihydro-[1,3]dioxolo[4,5-h]isoquinolino[2,1-b]isoquinolin-13-ium chloride
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~67.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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