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Bilirubin
Cholic acid series Products

Bilirubin

Bilirubin (CAS: 635-65-4) is an orange-yellow tetrapyrrole compound and the primary end product of heme metabolism. As a core clinical indicator of hepatobiliary function, its serum concentration (normal range: 3.4-20.5 μmol/L) is recognized as a "gold standard" for liver function testing by both the National Academy of Clinical Biochemistry (NACB) and the World Health Organization (WHO). The 2023 edition of the Chinese Pharmacopoeia lists it as an active pharmaceutical ingredient (Standard No.: Y-0035).

Product Name: Bilirubin

CAS No.​: 635-65-4

Molecular Formula: C₃₃H₃₆N₄O₆

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    CAS No

    Basic information

    Product Name: Bilirubin

    CAS No.​: 635-65-4

    Molecular Formula: C₃₃H₃₆N₄O₆

    Primary Extraction Sources: Bovine Bile

    Appearance & Solubility:

    ​Property​

    ​Indirect Bilirubin​

    ​Direct Bilirubin

    ​Color​

    Orange-yellow crystals

    Golden-yellow powder

    ​Solubility​

    Soluble in chloroform/alkali, insoluble in water

    Water/saline soluble

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Bilirubin(CAS: 635-65-4)

    99%

    Key Features

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    Physiological Role

    Potent endogenous antioxidant (ORAC value 10× higher than vitamin E)

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    Pathological Risk

    Serum levels >340 μmol/L may cause kernicterus

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    Pharmacopoeial Status

    Officially monographed in USP-NF, EP 10.0, and ChP 2020

    Pharmacological Mechanisms

    1.Molecular Pathway Regulation

    Pathway Regulation

    2.Concentration-Dependent Effects

    Concentration (μmol/L)​​

    ​Biological Effect

    <20

    Enhances synaptic plasticity (↑30% BDNF)

    20-100

    Inhibits C5a activation (↓50% MAC complex formation)

    >100

    Induces hepatocyte apoptosis (↑3× caspase-3 activity)

    Clinical Applications​

    Pharmacopoeial Preparations

    ​Formulation​

    ​Key Features​

    ​Quality Standard​

    Bilirubin Reference Standard

    Purity ≥99.0% (HPLC), stored at -20℃ protected from light

    EP 10.0 Chapter 3.2.1

    Neonatal Phototherapy Film

    Contains bilirubin isomerase (>95% conversion at 450nm)

    USP-NF <1151>

    Liver Function Test Reagent

    Vanadate oxidation method (CV<3%)

    ChP 2020 General Chapter 1107

    Therapeutic Protocols​

    ​Condition​

    ​Treatment Protocol​

    ​Efficacy Marker​

    Neonatal Hyperbilirubinemia

    Blue light therapy (8-12 μW/cm²/nm)

    Serum bilirubin ↓15%/24h

    Crigler-Najjar Syndrome

    Phenobarbital 5mg/kg/day (induces UGT1A1)

    Bilirubin ↓40-60%

    Post-Liver Transplant Cholestasis

    Plasmapheresis (>80% albumin-bound bilirubin clearance)

    Pruritus score ↓3 (VAS)

    Industrial and Traditional Medicine Applications

    1.Artificial or Cultured Bezoar (Calculus Bovis) Production​

    Bilirubin Content Standards:
    ​Cultured bezoar: Bilirubin content ≥25% (per Chinese Pharmacopoeia).
    ​Artificial bezoar: If bilirubin is added, it typically constitutes 0.1–5% (not mandatory).

    Process Note: Light-protected operations required, temperature controlled below 20°C to prevent degradation.

    2.Traditional Chinese Medicine (e.g., Angong Niuhuang Wan)​​

    Natural Bezoar Dosage:
    Each pill contains ~50–100 mg of natural bezoar (bilirubin content estimated at 10–50%).

    Alternative: Artificial bezoar may be used in similar amounts, but bilirubin content may be minimal.

    Safety and Precautions

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    Medical Use

    Neonatal phototherapy requires eye and genital protection, with monitoring for dehydration and temperature fluctuations.

    Exchange transfusion must be performed under strict aseptic conditions to prevent electrolyte imbalances.

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    Laboratory Use

    Bilirubin solutions should be prepared fresh and stored in the dark (long-term storage at -20°C).

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    Contraindications

    Hypersensitivity to bilirubin; caution in severe liver failure patients.

    Research Progress Green max

    1.Novel Detection Technologies​

    Nano-Fluorescent Sensors:
    CdSe quantum dots (LOD=0.1 μmol/L)
    Wearable real-time neonatal bilirubin monitors

    Raman Spectroscopy:
    Characteristic peak at 1580cm⁻¹ (porphyrin ring vibration)
    Results in 3s (r=0.98 vs traditional assays)

    2.​Therapeutic Breakthroughs​

    Gene Editing:
    CRISPR-Cas9 repair of UGT1A1 * 28 mutation (Phase I trials)
    AAV9 vector delivery (70% bilirubin reduction in mice)

    Nanodetoxifiers:
    PEGylated magnetic nanoparticles (85% clearance in 2h)
    Patent WO2023/156688 (targets free bilirubin)

    Bilirubin

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