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Genistein
Natural API

Genistein

Genistein (CAS: 446-72-0) is a naturally occurring isoflavone predominantly found in leguminous plants such as soybeans and red clover. As a representative phytoestrogen, it exhibits broad biological activities including antioxidant, anti-inflammatory, antitumor, and cardiovascular protective effects, making it a key target for functional food and pharmaceutical development.

Product Name: Genistein

IUPAC Name: 4',5,7-Trihydroxyisoflavone

CAS No.​: 446-72-0

Molecular Formula: C₁₅H₁₀O₅

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    Genistein

    Basic information

    Product Name: Genistein

    IUPAC Name: 4',5,7-Trihydroxyisoflavone

    CAS No.​: 446-72-0

    Molecular Formula: C₁₅H₁₀O₅

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    White crystalline powder

    ​Melting Point​

    297-300°C (decomposition)

    ​Solubility​

    Very low in water (<0.01 mg/mL), soluble in DMSO/ethanol

    ​logP​

    2.1 (moderate lipophilicity)

    ​pKa​

    7.2 (7-OH), 9.6 (4'-OH)

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Genistein  (CAS:446-72-0)

    98% by HPLC

    Loss on drying

    ≤1.0%

    Residue on ignition

    ≤1.0%

    Key Features

    index_10-7

    Natural Sources

    Soybeans (0.1-0.3%), red clover (0.5-1%).
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    Dual Activity

    Displays both estrogenic and anti-estrogenic properties.
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    High Safety

    Long history of dietary consumption with no significant toxicity.

    Pharmacological Mechanisms

    1.Molecular Target Network

    Pharmacological Mechanisms3

    2.Pharmacokinetics

    Absorption

    Low oral bioavailability (<10%), metabolized by gut microbiota.

    Distribution

    High in liver/lungs/breast; poor BBB penetration (<1%).

    Metabolism

    Hepatic glucuronidation (UGT1A1/1A9), hydroxylation (CYP1A2).

    Excretion

    Primarily biliary (80%), urinary excretion <5%

    Clinical Applications

    ​Indication​

    ​Mechanism​

    ​Stage

    ​Breast Cancer Adjuvant​

    ERβ agonism + anti-angiogenesis

    Phase II

    ​Menopausal Symptoms​

    Phytoestrogenic effects

    Marketed (supplement)

    ​Osteoporosis​

    Osteoblast differentiation

    Phase I

    Dosage and Administration

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    Anticancer

    300-600 mg/day (requires nanoformulations).
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    Menopause

    50-100 mg/day.
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    ​Dietary Supplement

    30-50 mg/day.

    Safety Evaluation

    Adverse Reactions​

    ​System​

    ​Incidence​

    ​Manifestations​

    Gastrointestinal

    5%

    Mild nausea

    Endocrine

    <1%

    Estrogenic effects

    Hypersensitivity

    Rare

    Rash

    Drug Interactions​

    CYP1A2 Substrates​ (e.g., caffeine): Metabolism slowed (AUC↑30%).

    Tamoxifen: Potential antagonism of anti-estrogen effects.

    Research Progress Green max

    Novel Formulations​

    Nanoemulsions: Bioavailability increased to 35%.

    Transdermal Patches: For localized estrogen therapy.

    New Indications​

    Alzheimer’s Disease: Reduces Aβ deposition (animal models).

    Diabetic Nephropathy: Inhibits TGF-β/Smad pathway.

    Sophora bean

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