ENMD-1068 hydrochloride|2703451-51-6|-陌孚医药/Medlife

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ENMD-1068 hydrochloride

目录号: PL10699 纯度: ≥98%

CAS No. :2703451-51-6

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中文名称	ENMD-1068 hydrochloride
英文名称	ENMD-1068 hydrochloride
英文别名	MS-24727;ENMD-1068 (hydrochloride);ENMD-1068 hydrochloride;2703451-51-6;HY-124748A;CS-0090095
Cas No.	2703451-51-6
分子式	C₁₅H₃₀ClN₃O₂
分子量	319.87
包装储存	4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情	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 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.
性状	Solid
IC50 & Target[1][2]	PAR2
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). ENMD-1068 (10 mM) inhibits trypsin or SLIGRL-NH2 stimulated calcium release in HSCs. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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)
参考文献	[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.

溶解度数据	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

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