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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.

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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.
Masse moléculaire

628.84

Formule

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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation
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Nom du produit:
12-O-Tiglyl-phorbol 13-dodecanoate
Cat. No.:
HY-N11736
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