For research use only. Not for therapeutic Use.
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[1][2].
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].
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].
| Catalog Number | I045834 |
| CAS Number | 2703451-51-6 |
| Synonyms | 6-amino-1-[4-(3-methylbutanoyl)piperazin-1-yl]hexan-1-one;hydrochloride |
| Molecular Formula | C15H30ClN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C15H29N3O2.ClH/c1-13(2)12-15(20)18-10-8-17(9-11-18)14(19)6-4-3-5-7-16;/h13H,3-12,16H2,1-2H3;1H |
| InChIKey | UDMQQSSIEIJEHG-UHFFFAOYSA-N |
| SMILES | CC(C)CC(=O)N1CCN(CC1)C(=O)CCCCCN.Cl |
| Reference | [1]. Sun Q, et al. ENMD-1068 inhibits liver fibrosis through attenuation of TGF-β1/Smad2/3 signaling in mice. Sci Rep. 2017 Jul 14;7(1):5498. doi: 10.1038/s41598-017-05190-7. Erratum in: Sci Rep. 2019 Dec 10;9(1):19125. [2]. Wang Y, et al. ENMD-1068, a protease-activated receptor 2 antagonist, inhibits the development of endometriosis in a mouse model. Am J Obstet Gynecol. 2014 Jun;210(6):531.e1-8. |
