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  3. 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.

12-O-Tiglyl-phorbol 13-dodecanoate

12-O-Tiglyl-phorbol 13-dodecanoate Chemical Structure

CAS No. : 37394-32-4

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Description

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[1].

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.

In Vivo

The 12-O-Tiglyl-phorbol 13-dodecanoate analog TD1 (5-20 mg/kg; p.o.; once every 2 days; 5 w) dose-dependently ameliorates carbon tetrachloride (HY-Y0298)-induced liver fibrosis in mice, with the efficacy at the 20 mg/kg dose comparable to that of 200 mg/kg Pirfenidone (HY-B0673)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice with Liver fibrosis (8-week-old male, carbon tetrachloride-induced liver fibrosis)[1]
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
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.
Molecular Weight

628.84

Formula

C37H56O8

CAS No.
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

Structure Classification
Initial Source
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Please store the product under the recommended conditions in the Certificate of Analysis.

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
12-O-Tiglyl-phorbol 13-dodecanoate
Cat. No.:
HY-N11736
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