12-O-Tiglyl-phorbol 13-dodecanoate
12-O-Tiglyl-phorbol 13-dodecanoate (TD13) is a potential inhibitor with anti-hepatic fibrosis activity, and it belongs to a series of derivatives of oral APOL2 inhibitors and anti-hepatic fibrosis agents. It shows no obvious toxicity in preclinical models. Compounds of the 12-O-Tiglyl-phorbol 13-dodecanoate series inhibit the expression of fibronectin, type I collagen and α-smooth muscle actin in hepatic stellate cells. 12-O-Tiglyl-phorbol 13-dodecanoate can be isolated from the Euphorbiaceae plant Euphorbia fischeriana, and it is applicable to the research of hepatic fibrosis.
For research use only. We do not sell to patients.
- CAS No.: 37394-32-4
- Formula: C37H56O8
- Molecular Weight:628.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Collagen I |
In Vitro
The 12-O-Tiglyl-phorbol 13-dodecanoate homologue TD1 (10 μM; 48 h) significantly inhibits fibronectin expression in TGF-β1-stimulated LX-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with Liver fibrosis (8-week-old male, carbon tetrachloride-induced liver fibrosis)[1]
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Dosage:12-O-Tiglyl-phorbol 13-dodecanoate analog TD1:
5 mg/kg; 10 mg/kg; 20 mg/kg -
Administration:p.o.; once every 2 days; 5 weeks
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Result:Reduced liver inflammatory cell infiltration and fibrous proliferation in a dose-dependent manner.
Decreased serum alanine aminotransferase, aspartate aminotransferase levels and liver hydroxyproline content in a dose-dependent manner.
Downregulated protein expression of fibronectin, type I collagen and α-smooth muscle actin in the liver in a dose-dependent manner.
Achieved therapeutic effect equivalent to 200 mg/kg pirfenidone at 20 mg/kg dose.
Chemical Information
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CAS No. 37394-32-4
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Molecular Weight 628.84
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Formula C37H56O8
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SMILES
CCCCCCCCCCCC(O[C@@]12[C@@]([C@@]3([H])[C@]([C@@H]([C@H]2OC(/C(C)=C/C)=O)C)([C@@]4([H])[C@](CC(CO)=C3)(C(C(C)=C4)=O)O)O)([H])C1(C)C)=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Fibrosis/Collagen Morphometry
Fibrosis and collagen morphometry is based on the quantitative visualization of fibrillar collagen deposition in tissue sections using histochemical stains such as Sirius Red (Picrosirius Red) or Masson's trichrome, followed by image-based or polarization-enhanced analysis to estimate collagen proportional area as a surrogate of extracellular matrix accumulation during fibrotic remodeling. Sirius Red combined with polarized light microscopy enhances detection of collagen fibers due to birefringence properties, enabling more specific visualization of collagen type I and III fibrils compared to conventional bright-field histology, while whole-section or region-restricted digital morphometry reduces field-selection bias in fibrosis assessment. Alternative quantitative approaches include second harmonic generation (SHG) and two-photon excited fluorescence microscopy, which enable label-free detection of fibrillar collagen and have been validated against histological staining and biochemica
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Collagen: Sirius Red Staining
Sirius Red or picrosirius red staining is a histochemical method for visualizing collagen-rich extracellular matrix in tissue sections, and collagen fibers are detected as red-stained structures under bright-field microscopy with enhanced birefringence under polarized light. Picrosirius red is useful for assessing total collagen organization, distribution, and fibrosis burden, but polarized color should not be interpreted as a definitive collagen type I versus type III readout because color is affected by fiber orientation, thickness, and packing.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
Masson’s Trichrome (collagen/trichrome staining) is a histological technique that differentially stains tissue compartments using sequential acidic dyes to distinguish collagen from muscle and cytoplasmic components based on dye affinity and tissue permeability differences, enabling visualization of fibrosis and connective tissue architecture in histological sections. The classical formulation typically uses Weigert's iron hematoxylin for nuclear staining, Biebrich scarlet-acid fuchsin for cytoplasm and muscle, and aniline blue (or light green variants) for collagen, producing a characteristic blue/green collagen signal contrasted against red cytoplasm and dark nuclei. The staining principle relies on selective displacement of smaller dye molecules by larger anionic dyes in collagen-rich regions under controlled acidified conditions, which enhances collagen-specific dye retention. This property makes the method widely used for fibrosis assessment in organs such as heart, liver, lung, a
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)