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

ENMD-1068 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 可通过抑制 TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 还能抑制子宫内膜细胞的增殖,并诱导病灶中上皮细胞的凋亡 (apoptosis)。ENMD-1068 可用于子宫内膜异位症、肝纤维化的研究。

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ENMD-1068 Chemical Structure

ENMD-1068 Chemical Structure

CAS No. : 789488-77-3

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

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]

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

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.
体内研究
(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]

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.
分子量

283.41

Formula

C15H29N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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.

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ENMD-1068
目录号:
HY-124748
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