ENMD-1068_product_DataBase

Bioactivity	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].
Invitro	ENMD-1068（10 mM；24 小时）阻断原代小鼠 HSC 中的 TGF-β1/Smad 信号传导（TGF-β1/Smad 信号通路在 HSC 激活和胶原蛋白生成中发挥着至关重要的作用）[1]。ENMD-1068 (10 mM) 抑制 HSC 中胰蛋白酶或 SLIGRL-NH2 刺激的钙释放[1]。 0 --> ENMD-1068 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	ENMD-1068（25、50 mg/kg；腹腔注射；每周两次，持续 4 周）抑制小鼠肝纤维化[1]。ENMD-1068（25、50 mg/kg；腹腔注射；每日一次，持续 5 天）可抑制子宫内膜异位症生长并以剂量依赖性方式抑制 IL-6 和 MCP-1 水平[2]。ENMD-1068（25、50 mg/kg；腹腔注射；每天一次，持续 5 天）会导致小鼠上皮细胞增殖减少，细胞凋亡指数增加[2]。 Animal Model:
Name	ENMD-1068
CAS	789488-77-3
Formula	C15H29N3O2
Molar Mass	283.41
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
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.

PeptideDB

ENMD-1068

CAS: 789488-77-3 F: C15H29N3O2 W: 283.41