Indirubin
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Basic information
Product Name: Indirubin
IUPAC Name: (2E)-2,2'-Bi(1H-indole)-3,3'-dione
CAS No.: 479-41-4
Molecular Formula: C₁₆H₁₀N₂O₂
Physicochemical Properties:
Parameter |
Value/Description |
Appearance |
Purple-red powder |
Melting Point |
356-358°C (decomposition) |
Solubility |
Poor in water (0.01 mg/mL), soluble in DMSO (50 mg/mL) |
logP |
3.1 (high lipophilicity) |
UV Characteristics |
λmax=540 nm (ε=12,000); purple-red in methanol |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
Indirubin (CAS: 479-41-4) |
98% by HPLC |
Loss on drying |
≤0.5% |
Residue on ignition |
≤0.5% |
Natural Source
Multi-Target Action
Low Toxicity
1. Molecular Target Network
2. Pharmacokinetics
Absorption
15% oral bioavailability (↑to 50% with liposomes).
Distribution
High in liver/spleen; low BBB penetration (<1%).
Metabolism
Hepatic CYP1A2 hydroxylation (forms 5-hydroxyindirubin).
Excretion
Primarily biliary (80% clearance in 72h).
Clinical Applications
Indications & Protocols
Condition |
Regimen |
Evidence |
Chronic Myeloid Leukemia |
50-100 mg tid ×6mo |
75% hematologic response* |
Psoriasis |
0.5% topical ointment bid |
↓50% PASI score |
Alzheimer’s Disease |
10 mg/kg (Phase II) |
MMSE improvement |
*Multicenter Phase III trial (n=300)
Special Populations
Hepatic Impairment: Reduce dose 30% (Child-Pugh B).
Pediatrics: ≥12 years (monitor CBC).
Dosage and Administration
Formulations
Tablets: 25 mg (film-coated).
Ointment: 0.5% w/w (petrolatum base).
Injection: 10 mg lyophilized powder (research use).
Dosing Guidelines
Use |
Dose |
Duration |
Leukemia |
75-150 mg/day |
6-12 months |
Dermatology |
Topical bid |
Until lesion clearance |
Cancer Prevention |
25 mg qd |
Long-term |
Safety Evaluation
Adverse Reactions
System |
Incidence |
Manifestations |
Gastrointestinal |
20% |
Nausea, diarrhea |
Hematologic |
5% |
Mild thrombocytopenia |
Dermatologic |
3% |
Hyperpigmentation |
Contraindications & Interactions
Absolute CI:
Pregnancy (teratogenic in animals).
Severe myelosuppression (ANC <1.5×10⁹/L).
Cautions:CYP1A2 inhibitors (e.g., fluvoxamine): ↑2× AUC.
Research Progress Green max
Novel Formulations
Nanocrystal Suspension: Oral bioavailability ↑to 40%.
Transdermal Patch: For psoriasis (Patent CN1148765).
New Indications
Triple-Negative Breast Cancer: Inhibits BRCA1-deficient cells (preclinical).
COVID-19: Blocks SARS-CoV-2 3CL protease (IC₅₀=8 μM).
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