Furamidine dihydrochloride (Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride)

目录号: HY-110137 纯度: ≥99.0%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

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Furamidine dihydrochloride Chemical Structure

CAS No. : 55368-40-6

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Customer Review

Other Forms of Furamidine dihydrochloride:

Furamidine 询价

MCE 顾客使用本产品发表的 2 篇科研文献

Furamidine dihydrochloride 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

生物活性
纯度 & 产品资料
参考文献

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^[1]^[2]^[3].

IC₅₀ & Target

PRMT1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
B16	IC₅₀	9.2 μM Compound: DB75	Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation	[PMID: 11985467]
HEK293	IC₅₀	178.04 μM Compound: 7e; DB75	Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay	[PMID: 28038325]
HEK-293T	IC₅₀	166 μM Compound: 1, DB75, furamidine	Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay	[PMID: 24564570]
L6	IC₅₀	23.3 μM Compound: FMD, DB75, Furamidine	Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs	[PMID: 23795673]
L6	IC₅₀	6.4 mM Compound: FMD	Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 23871911]
L6	IC₅₀	6.4 nM Compound: Furamidine	Cytotoxicity against rat L6 cells by alamar blue assay Cytotoxicity against rat L6 cells by alamar blue assay	[PMID: 17178177]
L6	IC₅₀	6.4 μM Compound: FMD, Furamidine	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24268543]
L6	IC₅₀	6.4 μM Compound: FMD, DB75, Furamidine	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 23795673]
L6	IC₅₀	6.4 μM Compound: FMD	Cytotoxicity against rat L6 cells by Alamar blue assay Cytotoxicity against rat L6 cells by Alamar blue assay	[PMID: 34146914]
L6	IC₅₀	6.4 μM Compound: Furamidine	Cytotoxicity against rat L6 cells by alamar blue assay Cytotoxicity against rat L6 cells by alamar blue assay	[PMID: 21194955]
L6	IC₅₀	6400 nM Compound: 2a	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24012380]

体外研究
(In Vitro)

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^[1]。
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^[1]。
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^[2]。

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

Cell Viability Assay^[1]

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^[1]

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；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^[3]。

MCE 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)^[3]
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.

分子量

377.27

Formula

C₁₈H₁₈Cl₂N₄O

CAS 号

55368-40-6

性状

固体

颜色

Light yellow to yellow

中文名称

呋喃脒二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 12.5 mg/mL (33.13 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

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); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.31 mM); 澄清溶液

此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: ≥99.0%

选择批次：

Data Sheet (644 KB) SDS (393 KB)

COA (285 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22. [Content Brief]

[2]. Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-84. [Content Brief]

[3]. Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67. [Content Brief]

Furamidine dihydrochloride 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6506 mL	13.2531 mL	26.5062 mL	66.2655 mL
	5 mM	0.5301 mL	2.6506 mL	5.3012 mL	13.2531 mL
	10 mM	0.2651 mL	1.3253 mL	2.6506 mL	6.6266 mL
	15 mM	0.1767 mL	0.8835 mL	1.7671 mL	4.4177 mL
	20 mM	0.1325 mL	0.6627 mL	1.3253 mL	3.3133 mL
	25 mM	0.1060 mL	0.5301 mL	1.0602 mL	2.6506 mL
	30 mM	0.0884 mL	0.4418 mL	0.8835 mL	2.2089 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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上海工商

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Furamidine dihydrochloride (Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride)

Customer Review

Other Forms of Furamidine dihydrochloride:

MCE 顾客使用本产品发表的 2 篇科研文献