呋喃脒二盐酸盐
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- CAS号:
- 55368-40-6
- 英文名:
- Furamidine dihydrochloride
- 英文别名:
- DB75;DB-75;WR-199385;Furamidine;Furamidine HCl;DB75 dihydrochloride;FuraMidine Dihydrochloride;Furamidine (hydrochloride);NSC 305831 dihydrochloride;DB 75, DB75, NSC 305831, WR199385
- 中文名:
- 呋喃脒二盐酸盐
- 中文别名:
- 呋喃脒二盐酸盐;呋喃二脒 二盐酸盐;化合物 T27395;DB75 DIHYDROCHLORIDE; NSC 305831 DIHYDROCHLORIDE
- CBNumber:
- CB51518554
- 分子式:
- C18H16N4O
- 分子量:
- 0
- MOL File:
- 55368-40-6.mol
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呋喃脒二盐酸盐化学性质
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熔点:
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400-401 °C(Solv: ethanol (64-17-5))
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储存条件:
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-20°C
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溶解度:
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DMSO (Slightly), Methanol (Slightly)
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形态:
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powder
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颜色:
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white to beige
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稳定性:
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Light Sensitive
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呋喃脒二盐酸盐性质、用途与生产工艺
Furamidine dihydrochloride (DB75 dihydrochloride) 是一种选择性的且细胞可渗透的蛋白精氨酸甲基转移酶 1 (PRMT1) 抑制剂,IC50 为 9.4 μM。Furamidine dihydrochloride 对 PRMT1 的选择性高于 PRMT5,PRMT6 和 PRMT4 (CARM1) (IC50 分别为 166 µM,283 µM 和 >400 µM)。Furamidine dihydrochloride 是一种有效的,可逆的和竞争性的酪氨酰 DNA 磷酸二酯酶 1 (TDP-1) 抑制剂。Furamidine dihydrochloride 对 TDP-1 的抑制作用对单链和双链 DNA 底物均有效,对双链 DNA 的作用更强。Furamidine dihydrochloride 也是一种抗寄生虫剂。
IC50: 9.4 μM (Protein arginine methyltransferase 1 (PRMT1)); 166 µM (PRMT5), 283 µM (PRMT6) and >400 µM (PRMT4)
Parasite
Tyrosyl-DNA phosphodiesterase 1 (TDP-1)
Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.
Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells.
Furamidine binds duplex DNA in the DNA minor groove selectively at AT rich sites [(A/T)4]. Furamidine can also intercalate between GC base pairs of duplex DNA. Furamidine could therefore interfere with DNA processing enzymes such as TDP-1.
Cell Viability Assay
Cell Line:
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Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
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Concentration:
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20 μM
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Incubation Time:
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72 hours
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Result:
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Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.
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Western Blot Analysis
Cell Line:
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293T cells
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Concentration:
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20 μM
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Incubation Time:
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15 hours
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Result:
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The expression level of the methylated GFP-ALY protein is significantly reduced.
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Furamidine (1 mg/kg; intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks; female NZB/NZW mice) and Irinotecan combined treatment suppresses proteinuria and prolongs survival of lupus-prone NZB/NZW mice. The combination treatment does not change the levels of anti-dsDNA antibodies.
Animal Model:
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Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)
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Dosage:
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1 mg/kg
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Administration:
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Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
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Result:
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Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.
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呋喃脒二盐酸盐
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-110137 | 呋喃脒二盐酸盐 Furamidine dihydrochloride | 55368-40-6 | 5mg | 1300元 |
2024/04/30 | HY-110137 | Furamidine dihydrochloride | | 25 mg | 4850元 |
55368-40-6, 呋喃脒二盐酸盐 相关搜索:
- Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Heterocycles
- Aromatics
- 高端化学
- C18H16N4O
- DB75 DIHYDROCHLORIDE; NSC 305831 DIHYDROCHLORIDE
- 呋喃二脒 二盐酸盐
- 化合物 T27395
- 呋喃脒二盐酸盐
- 55368-40-6
- DB75 dihydrochloride
- NSC 305831 dihydrochloride
- DB 75, DB75, NSC 305831, WR199385
- Furamidine (hydrochloride)
- 4,4'-(2,5-Furandiyl)bis-benzenecarboximidamide dihydrochloride
- Furamidine dihydrochloride >=98% (HPLC)
- 4,4'-(Furan-2,5-diyl)dibenzimidamide dihydrochloride
- Furamidine HCl
- FuraMidine Dihydrochloride
- WR-199385
- 4-[5-(4-carbamimidoylphenyl)-2-furyl]benzenecarboximidamide
- Furamidine
- DB-75
- DB75
- 2,5-Furandiylbis(1,4-phenylene)bisformamidine