Taurohyodeoxycholic acid sodium salt hydrate
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Basic information
Product Name: Taurohyodeoxycholic acid sodium salt hydrate
CAS No.: 38411-85-7
Molecular Formula: C₂₆H₄₄NNaO₆S
IUPAC Name: Sodium (2S)-2-[[(3α,5β,6α)-3,6-dihydroxy-24-oxocholan-24-yl]amino]ethanesulfonate monohydrate
Appearance & Solubility:
Property |
Specification |
Appearance |
White hygroscopic crystalline powder |
Melting Point |
>265°C (decomposition) |
Water Solubility |
550 mg/mL (25°C) |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
| Taurohyodeoxycholic acid sodium salt hydrate (CAS: 38411-85-7) | 99% |
Structural Uniqueness
6α-hydroxyl configuration (rare in mammalian bile acids)
Functional Advantages
40% stronger cholesterol solubilization than UDCA sodium salt (in vitro)
Unique immunomodulation (↓55% IL-1β secretion)
Pharmacopoeial Standards
USP-NF requires ≥98.5% purity
ChP 2025 limits total impurities ≤1.0%
Applications
Therapeutic Uses
Hepatobiliary Diseases:
Cholesterol gallstones (72% dissolution rate at 18 months)
Cholestatic liver disease (ALP↓45%, GGT↓38%)
Metabolic Disorders:
Non-alcoholic fatty liver (↓35% hepatic fat content by MRI-PDFF)
Industrial Applications
Field |
Application |
Representative Products |
Pharmaceutical Excipients |
Solubilizer for poorly soluble drugs |
Sirolimus nanosuspension |
Diagnostic Reagents |
Bile acid profiling internal standard |
UPLC-MS/MS calibrant |
1. Gallstone Dissolution Mechanism
2. Molecular Targets
Target |
Effect |
EC50 |
FXR Nuclear Receptor |
↑2× transcriptional activity |
20 μM |
TGR5 Receptor |
↑150% GLP-1 secretion |
50 μM |
Formulations
Form |
Specification |
Features |
Enteric-coated Pellets Capsule |
300mg/capsule |
Gastric acid-resistant |
Lyophilized Powder for Injection |
250mg/vial |
Reconstitute with 5% glucose |
Dosing Regimens
Indication |
Dose |
Duration |
Gallstones |
15 mg/kg/d |
18-24 months |
Severe Cholestasis |
8 mg/kg/d IV |
5-7 days |
Safety Profile
Adverse Reactions
System |
Effect (Incidence) |
Management |
Gastrointestinal |
Diarrhea (18%) |
Dose reduction/split dosing |
Dermatological |
Rash (4%) |
Antihistamine treatment |
Drug Interactions
Synergistic Effects: With PPARγ agonists (lipid-lowering synergy)
Contraindicated Combinations: Cation exchange resins (>95% adsorption)
Research Progress Green max
1. Novel Formulations
● Nanostructured Lipid Carriers:
85±5 nm particle size, ↑75% liver targeting efficiency
● Colon-Targeted Delivery System:
Azoreductase-triggered release (ileocecal pH>7)
2.Emerging Indications
● Atherosclerosis:
↓40% aortic plaque area (ApoE-/- mouse model)
● Type 2 Diabetes:
↑25% β-cell function (HOMA-β)
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