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Chenodeoxycholic acid
Cholic acid series Products
Chenodeoxycholic acid.jpg
CAS No.​ 474-25-9.jpg

Chenodeoxycholic acid

Chenodeoxycholic acid (CDCA, CAS: 474-25-9) is a primary bile acid with the chemical formula C₂₄H₄₀O₄ and molecular weight 392.57 g/mol. As a major component of human bile (30-40% of bile acid pool), it is FDA-approved as a cholesterol gallstone dissolving agent (brand name: Chenodal®). The 2023 EASL guidelines list it as a second-line therapy for primary biliary cholangitis (PBC) (Evidence Level: 1B).

Product Name: Chenodeoxycholic acid

CAS No.​: 474-25-9

Molecular Formula: C₂₄H₄₀O₄

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    CAS No

    Basic information

    Product Name: Chenodeoxycholic acid

    CAS No.​: 474-25-9

    Molecular Formula: C₂₄H₄₀O₄

    IUPAC Name: (3α,5β,7α)-3,7-Dihydroxycholan-24-oic acid

    Appearance & Solubility:

    Property​

    ​Specification​

    Appearance

    White crystalline powder

    Melting Point

    165-167°C

    Water Solubility

    0.1 mg/mL (free acid)

    0.1M NaOH Solubility

    400 mg/mL

    Quality Standard: CP2020,JP,Customer Made

    Specification

    Test Items

    Standard

    Chenodeoxycholic acid(CAS: 474-25-9)

    90%-98%

    Key Features

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    Structural Features

    3α,7α-dihydroxy-5β-cholan-24-oic acid (lacks 12α-hydroxyl group)

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    Functional Properties

    Physiological concentration (1-10 μM): Promotes cholesterol solubilization (↓40% bile cholesterol saturation)

    High concentration (>50 μM): Cytotoxic (induces apoptosis via mitochondrial pathway)

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    Pharmacopoeial Standards

    USP-NF, EP 11.0 and JP 18 require ≥98.0% purity

    Applications

    Therapeutic Uses​

    Gallstone Treatment:
    Dissolves cholesterol stones (60-80% efficacy at 6 months)
    Prevents stone recurrence (↓50% 5-year recurrence rate)

    Metabolic Disorders:Treatment of cerebrotendinous xanthomatosis (CTX, orphan drug designation)

    Industrial Applications​

    ​Field​

    ​Application​

    ​Representative Products​

    Pharmaceutical Excipients

    Enteric formulation solubilizer

    Cyclosporine soft capsules

    Cosmetics

    Skin barrier repair agent

    Medical repair creams

    Pharmacological Mechanisms

    1.Molecular Pathway Regulation

    Pharmacological Mechanisms

    2.Molecular Targets​

    ​Target​

    ​Effect​

    ​EC50​

    FXR Nuclear Receptor

    Upregulates BSEP transporter expression

    10 μM

    GPBAR1

    Stimulates bile secretion

    50 μM

    Clinical Applications

    Diagnostic Indicators

    ​Test​

    ​Clinical Significance​

    ​Reference Range​

    Total Bile Acids (TBA)

    Hepatobiliary function assessment

    0-10 μmol/L

    Bile Acid Profiling

    Etiological diagnosis of cholestasis

    Abnormal component ratios

    Therapeutic Protocols​

    Inborn Errors of Bile Acid Synthesis:Cholbam®: 10-15mg/kg/day in divided doses

    Biliary Atresia:Adjunct therapy to improve bile flow

    Clinical Applications​

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    Benefits
    Indications

    Cholesterol Gallstones:Oral 15mg/kg/day (6-24 months treatment)

    PBC:Combined with UDCA (250mg tid)
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    Benefits
    Contraindications​

    Pigment gallstones

    Acute cholecystitis

    Dosage & Administration

    Formulations​

    ​Form​

    ​Specification​

    ​Features​

    Tablets

    250mg/tablet

    Enteric-coated

    Capsules

    150mg/capsule

    MCT oil carrier

    Dosing Regimens​

    Indication​

    ​Dose​

    ​Duration​

    Gallstones

    15mg/kg/day

    6-24 months

    CTX

    750mg/day

    Lifelong therapy

    Safety Profile

     Adverse Reactions​

    System​

    ​Effect (Incidence)​​

    ​Management​

    Gastrointestinal

    Diarrhea (30%)

    Dose reduction/split dosing

    Hepatobiliary

    Elevated liver enzymes (5%)

    Discontinuation (reversible)

    Drug Interactions​

    Enhanced Effects: Requires 20% dose reduction when combined with statins

    Contraindicated Combinations: Aluminum preparations (↓90% absorption)

    Research Progress Green max

    Novel Formulations​

    Nanoemulsions:
    Soybean phospholipid carrier (↑60% bioavailability)

    Sustained-Release Pellets:
    Ethyl cellulose coating (12-hour release)

    New Indications​

    Non-Alcoholic Fatty Liver:
    Activates FXR/SHP pathway (↓40% steatosis in animal models)

    Inflammatory Bowel Disease:
    Modulates Th17/Treg balance (Phase II trials)

    Chenodeoxycholic acid

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