计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
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). ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 . 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ICR mice (8-week-old; CCl 4 -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.
Form:Solid
IC50& Target:PAR2
规格
别名
ENMD-1068盐酸盐
规格或纯度
≥98%
英文名称
ENMD-1068 hydrochloride
生化机理
ENMD-1068 盐酸盐是一种选择性蛋白酶激活受体 2（PAR2）拮抗剂。ENMD-1068 盐酸盐通过抑制 TGF-β1/Smad 信号传导，减少肝星状细胞活化和胶原表达。ENMD-1068盐酸盐还可抑制TGF
储存条件
2-8°C储存
运输条件
低温运输
作用类型
拮抗剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
319.87
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 200 mg/mL (625.25 mM; Need ultrasonic) H2O : 100 mg/mL (312.63 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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