Cholic acid
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Basic information
Product Name: Cholic acid
CAS No.: 81-25-4
Molecular Formula: C₂₄H₄₀O₅
IUPAC Name: (3α,5β,7α,12α)-3,7,12-Trihydroxycholan-24-oic acid
Physical Properties:
Property |
Specification |
Appearance |
White crystalline powder |
Melting Point |
197-202°C (decomposition) |
Solubility in Water |
0.15 mg/mL (25°C) |
Solubility in Ethanol |
35 mg/mL |
logP |
1.8 |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
Cholic acid(CAS: 81-25-4) |
99% |
Physiological Functions
Fat Metabolism
Form mixed micelles (3-10 nm diameter), enhancing lipase activity by 300%
Facilitate absorption of fat-soluble vitamins (A/D/E/K)
Cholesterol Regulation
Promote cholesterol excretion (bile acid/cholesterol secretion ratio 20:1)
Signaling
Therapeutic Uses
Field |
Application |
Product Examples |
Pharmaceuticals |
Drug solubilizer (for BCS Class II drugs) |
Cyclosporine soft capsules |
Cosmetics |
Transdermal absorption enhancer |
Premium serums |
Animal Feed |
Fat digestion promoter |
Piglet milk replacer |
1.Molecular Pathway Regulation
2.Concentration-Dependent Effects
Concentration (μmol/L) |
Biological Effect |
<10 |
Promote fat absorption |
10-40 |
Activate FXR pathway (inhibit bile acid synthesis) |
>40 |
Induce hepatocyte apoptosis (↑3× caspase-3) |
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
Dosage & Administration
Drug Formulations
Form |
Specification |
Features |
Capsules |
250mg/capsule (UDCA) |
Enteric-coated (acid-resistant) |
Tablets |
5mg/tablet (OCA) |
Administered on empty stomach |
Injection |
100mg/10mL (sodium cholate) |
Biliary drainage replacement |
Dosing Regimens
Indication |
Drug |
Dosage |
Primary Biliary Cholangitis |
UDCA |
13-15mg/kg/day in 2 doses |
Non-Alcoholic Fatty Liver |
OCA |
5mg once daily (titrate up) |
Bile Acid Diarrhea |
Colesevelam |
3.75g twice daily before meals |
Safety and Precautions
Adverse Reactions
Drug |
Common Side Effects (Incidence) |
Management |
UDCA |
Diarrhea (10%), pruritus (5%) |
Dose reduction/split dosing |
OCA |
Pruritus (30%), elevated LDL (15%) |
Combine with statins |
Bile Acid Sequestrants |
Constipation (25%), bloating (10%) |
Increase dietary fiber |
Contraindications
Absolute:
Complete biliary obstruction (UDCA/OCA)
Hypersensitivity to bile acid derivatives
Relative: Advanced cirrhosis (OCA may worsen pruritus)
Research Progress Green max
1. Novel Therapies
● FXR-Targeted Drugs:
Non-steroidal FXR agonists (TERN-101, Phase III trials)
Gut-selective FXR modulators (reduce systemic side effects)
● Microbiome Interventions:
Fecal microbiota transplantation (modulate secondary bile acid production)
2. Detection Technologies
● Mass Spectrometry Imaging:
MALDI-TOF visualization of hepatic bile acid distribution
● Microfluidic Chips:
Finger-prick blood testing (5μL sample, CV<5%)
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