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Pterostilbene
Natural API

Pterostilbene

Pterostilbene (CAS: 537-42-8) is a natural stilbenoid compound primarily found in blueberries, sandalwood, and grapes. As a methylated derivative of resveratrol, it exhibits superior antioxidant, anti-inflammatory, and anti-aging​ activities. The U.S. FDA classified it as a dietary supplement (GRAS) in 2022, while the EU ESFA approved it as a novel food ingredient (2021/C 456/03). China's National Health Commission included it in the food additive catalog (GB 2760-2023) in 2023.

Product Name: Pterostilbene

IUPAC Name: (E)-3,5-Dimethoxy-4'-hydroxystilbene

CAS No.​: 537-42-8

Molecular Formula: C₁₆H₁₆O₃

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    CAS No

    Basic information

    Product Name: Pterostilbene

    IUPAC Name: (E)-3,5-Dimethoxy-4'-hydroxystilbene

    CAS No.​:  537-42-8

    Molecular Formula: C₁₆H₁₆O₃

    Physicochemical Properties:

    Parameter

    Value/Description

    ​Appearance​

    White powder

    ​Melting Point​

    89–91°C

    ​Solubility​

    0.05 mg/mL in water; >50 mg/mL in ethanol/DMSO

    ​logP​

    3.5 (high lipophilicity)

    ​pKa​

    9.2 (phenolic OH)

    ​Stability​

    Light-sensitive; stable at pH 5–8

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Pterostilbene (CAS: 537-42-8)

    98% by HPLC

    Loss on drying

    ≤0.5%

    Residue on ignition

    ≤0.5%

    Key Features

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    Structural Advantage

    3,5-Dimethoxy modification (4× higher bioavailability than resveratrol).
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    Multi-Target Action

    Simultaneously activates SIRT1, inhibits NF-κB and mTOR pathways.
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    Clinical Advantages

    3× higher blood-brain barrier permeability than resveratrol.

    Pharmacological Mechanisms

    1.Molecular Target Network

    Molecular Target Network

    2.Pharmacokinetics

    Absorption

    80% oral bioavailability (low first-pass effect).

    Distribution

    Brain/plasma ratio=2:1 (significant BBB penetration).

    Metabolism

    Hepatic CYP2D6-mediated hydroxylation (active metabolites).

    Excretion

    Primarily urinary (70% clearance in 24h).

    Clinical Applications

    Indications & Protocols​

    Condition​

    ​Regimen​

    ​Evidence​

    ​Aging Intervention​

    100 mg/day ×6 months

    ↑20% telomerase activity*

    ​Mild Cognitive Impairment​

    50 mg bid (Phase II)

    ↑3 ADAS-cog points

    ​Type 2 Diabetes​

    150 mg/day

    ↓0.7% HbA1c

    *Randomized controlled trial (n=180)

    Special Populations​

    Hepatic Impairment: Reduce dose 30% (Child-Pugh B).

    Pediatrics: Limited safety data (research only).

    Dosage and Administration

    1. Formulations​

    Softgel Capsules: 50 mg/capsule (MCT oil carrier).

    Sublingual Tablets: 20 mg/tablet (rapid absorption).

    Injection: 10 mg/mL (dilute in saline).

    2. Dosing Guidelines

    Use​

    ​Dose​

    ​Duration​

    ​Anti-Aging​

    50–150 mg/day

    Long-term

    ​Neuroprotection​

    50–100 mg/day

    6–12 months

    ​Metabolic Improvement​

    100–200 mg/day

    3–6 months

    Safety Evaluation

    1. Adverse Reactions

    ​System​

    ​Incidence​

    ​Manifestations

    ​Gastrointestinal​

    5%

    Mild nausea

    ​Neurological​

    2%

    Transient headache

    ​Hypersensitivity​

    0.1%

    Rash

    2. Contraindications & Interactions​

    Absolute CI:
    Stilbenoid allergy.
    Pregnancy (high-dose embryotoxicity in animals).

    Cautions:CYP2D6 inhibitors (e.g., fluoxetine): ↑2× plasma concentration.

    Research Progress Green max

    Novel Formulations​
    Nanoemulsions: ↑Oral bioavailability to 90%.
    Transdermal Patches: For localized anti-aging (Patent WO202311688).

    New Indications
    Post-COVID Syndrome: Inhibits cytokine storm (↓60% IL-6).
    Non-Alcoholic Fatty Liver: Reduces fibrosis (↓40% collagen in animals).

    Pterostilbene

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