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编 号:F754772
分子式:C15H30ClN3O2
分子量:319.87
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体内研究:
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。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。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。Animal Model:ICR mice (8-week-old; CCl4-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.

体外研究:
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)。ENMD-1068 (10 mM) 抑制 HSC 中胰蛋白酶或 SLIGRL-NH2 刺激的钙释放。
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