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Puerarin 5-HT Receptor antagonist

Cat.No.S2346

Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.
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Quality Control

Batch: S234601 DMSO]86 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.80%
99.80

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (206.54 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 416.38 Formula

C21H20O9

Storage (From the date of receipt)
CAS No. 3681-99-0 Download SDF Storage of Stock Solutions

Synonyms Kakonein SMILES C1=CC(=CC=C1C2=COC3=C(C2=O)C=CC(=C3C4C(C(C(C(O4)CO)O)O)O)O)O

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Mechanism of Action

In vitro
Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. This compound is employed clinically to treat cardiovascular diseases in China. Another study showed that this chemical also possessed anti-cancer properties. It at 25 μM dose-dependently reduces HT-29 cellular growth with an increase of bax and decreases of c-myc and bcl-2.
In vivo
In hypercholesterolmic diet plus administration of puerarin (300 mg/kg/day, p.o.) rats, this compound markedly attenuated the increased total cholesterol induced by hypercholesterolmic diet in both serum and liver. LD50: Mice 738mg/kg (i.v.)
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-05-21)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06968208 NOT_YET_RECRUITING
Metabolic Diseases; Obesity/Therapy
Ruijin Hospital
2025-08-01 PHASE2
NCT03676296 COMPLETED
Cardiovascular Disease Risk Factors
The University of Hong Kong
2018-09-05 PHASE2
NCT03099590 COMPLETED
Alcohol Drinking; Alcohol Use Disorder; Alcohol Abstinence
Mclean Hospital
2018-01-01 PHASE2
NCT02219191 UNKNOWN
Rheumatoid Arthritis
Chengdu PLA General Hospital
2014-08
NCT02264301 UNKNOWN
Rheumatoid Arthritis
Chengdu PLA General Hospital
2014-08
NCT02254655 COMPLETED
Rheumatoid Arthritis
Chengdu PLA General Hospital
2013-11 PHASE2

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