ENMD-1068 hydrochloride is a selective protease-activated receptor 2 ( PAR2 ) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis
In Vitro
ENMD-1068 (10 mM; 24 h) blocks TGF-β1/Smad signaling in primary mouse HSCs (TGF-β1/Smad signal pathway plays a crucial role in HSCs activation and collagen production). ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Hepatic stellate cells (HSCs) (TGF-β1-stimulated) Concentration: 10 mM Incubation Time: 24 h Result: Inhibited TGF-β1-induced expression of α-SMA, Col α1(І),Col α1(III), and Smad2/3 C-terminal phosphorylation.
In Vivo
ENMD-1068 (25, 50 mg/kg; i.p.; twice per week for 4 weeks) inhibits liver fibrosis of mice . ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) inhibits endometriosis growth and suppresses the levels of IL-6 and MCP-1 in a dose-dependent manner. ENMD-1068 (25, 50 mg/kg; i.p.; single daily for 5 days) causes a decrease in epithelial cell proliferation and an increase in the apoptotic index in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ICR mice (8-week-old; CCl 4 -induced liver fibrosis model) . Dosage: 25, 50 mg/kg Administration: Intraperitoneal injection; twice per week for 4 weeks Result: Markedly attenuated collagen deposition. Animal Model: Mice with surgically induced endometriosis. Dosage: 25, 50 mg/kg Administration: Intraperitoneal injection; single daily for 5 days Result: Reduced the volume of observed lesions in a dose-dependent manner. Inhibited the expression of IL-6 and MCP-1. Decreased the proliferation rate of endometriotic cells and increased the percentage of apoptotic epithelial cells in the lesions.
Form:Solid
IC50& Target:PAR2
Names and Identifiers
Canonical SMILES
O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN.Cl
Molecular Weight
319.87
Certificates
Certificate of Analysis(COA)
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Chemical and Physical Properties
Solubility
DMSO : 200 mg/mL (625.25 mM; Need ultrasonic) H2O : 100 mg/mL (312.63 mM; Need ultrasonic)
