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编 号:F388289
分子式:C18H18Cl2N4O
分子量:377.27
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5mg
1950
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10mg
3300
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25mg
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50mg
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生物活性:
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.

体内研究:
Furamidine (1 mg/kg;腹膜内注射;每周 3 次,每 4 周重复一次;持续 34 周;雌性 NZB/NZW 小鼠) dihydrochloride 和 Irinotecan 联合处理可抑制蛋白尿并延长易患狼疮的 NZB/NZW 小鼠的存活期。联合处理不会改变抗 dsDNA 抗体的水平。Animal Model:Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)
Dosage:1 mg/kg
Administration:Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
Result:Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.

体外研究:
Furamidine (Compound 1;20 μM;72 小时;白血病细胞系) dihydrochloride 抑制除具有 JAK2V617F 突变的 HEL 细胞外的大多数白血病细胞系的细胞生长。 Furamidine (20 μM;15 小时;293T 细胞) dihydrochloride 处理显著降低 293T 细胞中甲基化 GFP-ALY 蛋白的表达水平。 Furamidine dihydrochloride 也可以插入双链 DNA 的 GC 碱基对之间。因此,Furamidine dihydrochloride 可能会干扰 DNA 加工酶,例如 TDP-1。
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