ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride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 hydrochloride 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。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。
| 生物活性 | ENMD-1068 hydrochloride is a selectiveprotease-activated receptor2(PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibitingTGF-β1/Smadsignaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and inducesapoptosisof epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis[1][2]. |
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体外研究
(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)[1].
ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs[1].
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(?),Col α1(III), and Smad2/3 C-terminal phosphorylation. |
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体内研究
(In Vivo) | 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].
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(625.25 mM;Need ultrasonic) H2O : 100 mg/mL(312.63 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.1263 mL | 15.6314 mL | 31.2627 mL | | 5 mM | 0.6253 mL | 3.1263 mL | 6.2525 mL | | 10 mM | 0.3126 mL | 1.5631 mL | 3.1263 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 100 mg/mL (312.63 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 5 mg/mL (15.63 mM); Suspended solution; Need ultrasonic
此方案可获得 5 mg/mL (15.63 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (15.63 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (15.63 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (15.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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