S81389 |
SGC707 |
源叶(MedMol) | 98% |
- 提示:详情请下载说明书。
- 产品描述: SGC707 is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC50=31 nM, Kd=53 nM).
- 靶点: PRMT3:31 nM (IC50);HistoneMethyltransferase
- 体外研究:
SGC707 (0-10 μM; 6 h) binds to PRMT3 in both HEK293 and A549 cells. Cell Viability Assay Cell Line: HEK293 and A549 cells Concentration: 0-10 μM Incubation Time: 6 hours Result: Stabilized PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively.
- 体内研究:
SGC707 (intraperitoneal injection; 10 mg/kg; 3 times per week; 3 w) treatment reduces hepatic steatosis and plasma triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Animal Model: Western-type diet-fed LDL (lipoprotein) receptor knockout mice Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; 3 times per week; 3 weeks Result: Exhibited 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels.
- 参考文献:
1. Kaniskan HÜ, et al. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. 2. de Jong LM, et al. PRMT3 inhibitor SGC707 reduces triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Sci Rep. 2022 Jan 10;12(1):483.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.352 ml 16.759 ml 33.519 ml 5 mM 0.67 ml 3.352 ml 6.704 ml 10 mM 0.335 ml 1.676 ml 3.352 ml 50 mM 0.067 ml 0.335 ml 0.67 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)