2. GPCR/G Protein Apoptosis
  3. Protease Activated Receptor (PAR) Apoptosis
  4. ENMD-1068

ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis.

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ENMD-1068 Chemical Structure

ENMD-1068 Chemical Structure

CAS No. : 789488-77-3

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ENMD-1068 Related Antibodies

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Description

ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis[1][2].

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)[1].
ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs[1].

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

ENMD-1068 Related Antibodies

Western Blot Analysis[1]

Cell 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[1].
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[2].
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[2].

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

Animal Model: ICR mice (8-week-old; CCl4-induced liver fibrosis model)[1].
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[2].
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.
Molecular Weight

283.41

Formula

C15H29N3O2
CAS No.
SMILES

O=C(N1CCN(C(CC(C)C)=O)CC1)CCCCCN
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ENMD-1068 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

ENMD-1068789488-77-3ENMD1068ENMD 1068Protease Activated Receptor (PAR)ApoptosisThrombin receptorsendometriosisliver fibrosisHSCsIL-6NF-κBanti-proliferationMCP-1Inhibitorinhibitorinhibit

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