Furamidine dihydrochloride DB75 dihydrochloride; NSC 305831 dihydrochloride|cas:55368-40-6|西域试剂

Furamidine dihydrochloride DB75 dihydrochloride; NSC 305831 dihydrochloride,99.0%

产品编号：Bellancom-110137| CAS NO：55368-40-6| 分子式：C₁₈H₁₈Cl₂N₄O| 分子量：377.27

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-110137		￥2600.00	杭州北京（现货）

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Furamidine dihydrochloride DB75 dihydrochloride; NSC 305831 dihydrochloride

产品介绍

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。

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
Concentration:	20 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.

Western Blot Analysis

Cell Line:	293T cells
Concentration:	20 μM
Incubation Time:	15 hours
Result:	The expression level of the methylated GFP-ALY protein is significantly reduced.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 12.5 mg/mL (33.13 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6506 mL	13.2531 mL	26.5062 mL
5 mM	0.5301 mL	2.6506 mL	5.3012 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.25 mg/mL (3.31 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.31 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 12.5 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.25 mg/mL (3.31 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.31 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。