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Suramin hexasodium salt

(Synonyms: 苏拉明钠; Suramin hexasodium salt)

目录号: PC12209 纯度: ≥98%

P2嘌呤拮抗剂,Suramin sodium salt是具有多种生物活性的多磺化萘基脲。Suramin是DNA拓扑异构酶II抑制剂，IC50为5 μM。

CAS No. :129-46-4

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中文名称	Suramin hexasodium salt
中文别名	苏拉明钠;8,8'-碳酰双亚氨-3,1-亚苯基碳酰亚氨-(4-甲基-3,1-亚苯基)碳酰亚氨双-1,3,5-萘三磺酸六钠;苏拉明;舒拉明钠;苏拉林;蘇拉明鈉;苏拉明钠盐
英文名称	Suramin hexasodium salt
英文别名	Suramin sodium;8,8'-Carbonylbisimino-3,1-phenylenecarbonylimino-(4-methyl-3,1-phenylene)carbonyliminobis-1,3,5-naphthalenetrisulfonic acid hexasodium;Suramin hexasodium salt;Suramin (Sodium Salt);SURAMIN HEXASODIUM SALT(RG);BAY-205;hexasodium,8-[[4-methyl-3-[[3-[[3-[[2-methyl-5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]phenyl]carbamoyl]phenyl]carbamoylamino]benzoyl]amino]benzoyl]amino]naphthalene-1,3,5-trisulfonate;NF-060;Suramin sodium salt;Suramin. Hexasodium Salt;Suramine sodium salt;8,8'-[CARBONYLBIS[IMINO-3,1-PHENYLENECARBONYLIMINO(4-METHYL-3,1-PHENYLENE)CARBONYLIMINO]]BIS-1,3,5-NAPHTHALENETRISULFONIC ACID HEXASODIUM SALT;309f;nf060;F-309;bay205;naganin;moranyl;SURAMIN;Naganol;naganine;bayer205
Cas No.	129-46-4
分子式	C₅₁H₃₄N₆Na₆O₂₃S₆
分子量	1429.17
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
详情描述	P2嘌呤拮抗剂,Suramin sodium salt是具有多种生物活性的多磺化萘基脲。Suramin是DNA拓扑异构酶II抑制剂，IC50为5 μM。

生物活性

Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

性状

Solid

IC50 & Target[1][2]

SIRT1

297 nM (IC₅₀)

SIRT2

1.15 μM (IC₅₀)

SIRT5

22 μM (IC₅₀)

体外研究(In Vitro)

Suramin sodium salt (Suramin hexasodium salt; 50-600 μg/mL; for 24-96 hours) inhibits cells proliferation in a dose-dependent and time-dependent manner and decreases viability in cancer cells.
Suramin sodium salt (300 μg/mL; for 48 hours) induces cells apoptosis and down-regulates mRNA expression in HeLa cells.
Suramin sodium salt (1 mg/mL; 1 hour) significantly suppresses the phosphorylated ERK1/2.
The IC₅₀ values of HO-8910 PM and HeLa are 319 μg/mL, 476 μg/mL, respectively.
Suramin blocks viral replication in Vero E6 cells.

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

Cell Proliferation Assay

Cell Line:	HO-8910 PM ovarian and Hela cervical cancer cells
Concentration:	50, 100, 200, 300, 400, 500 and 600 μg/mL
Incubation Time:	For 24, 48, 72 and 96 hours
Result:	Inhibited cells proliferation in a dose-dependent and time-dependent manner.

Apoptosis Analysis

Cell Line:	HeLa cells
Concentration:	300 μg/mL
Incubation Time:	For 48 hours
Result:	Induced cells apoptosis.

Western Blot Analysis

Cell Line:	PA-SMCs cells
Concentration:	1 mg/mL
Incubation Time:	For 1 hour
Result:	Significantly suppressed the phosphorylated ERK1/2.

体内研究(In Vivo)

Suramin sodium salt (Suramin hexasodium salt; 10 mg/kg; IV; twice weekly for 3 weeks) reverses established pulmonary hypertension (PH), thereby normalizing the pulmonary artery pressure values and vessel structure.

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

Animal Model:	Adult male Wistar rats (200-225 g)
Dosage:	10 mg/kg
Administration:	IV; twice weekly for 3 weeks
Result:	Reversed established PH, thereby normalizing the pulmonary artery pressure values and vessel structure.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

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

ClinicalTrial

参考文献

[1]. Zhang YL, et al. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998 May 15;273(20):12281-7. [Information]

[2]. Trapp J, et al. Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins). ChemMedChem. 2007 Oct;2(10):1419-31. [Information]

[3]. Schuetz A, et al. Structural basis of inhibition of the human NAD-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89. [Information]

[4]. De Clercq E, et al. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett. 1979 Nov;8(1):9-22. [Information]

[5]. Wanchao Yin, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol. 2021 Mar;28(3):319-325. [Information]

[6]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7. [Information]

[7]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375. [Information]

[8]. Novaes RD, et al. Purinergic Antagonist Suramin Aggravates Myocarditis and Increases Mortality by EnhancingParasitism, Inflammation, and Reactive Tissue Damage in Trypanosoma cruzi-Infected Mice. Oxid Med Cell Longev. 2018 Sep 30;2018:7385639. [Information]

[9]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073. [Information]

溶解度数据

体外研究:

DMSO : 83.33 mg/mL (58.31 mM; Need ultrasonic)

H₂O : 50 mg/mL (34.99 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.6997 mL	3.4985 mL	6.9971 mL
5 mM	0.1399 mL	0.6997 mL	1.3994 mL
10 mM	0.0700 mL	0.3499 mL	0.6997 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (69.97 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (1.46 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (1.46 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (1.46 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Zhang YL, et al. Suramin is an active site-directed, reversible, and tight-binding inhibitor of protein-tyrosine phosphatases. J Biol Chem. 1998 May 15;273(20):12281-7. [Information]

[2]. Trapp J, et al. Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins). ChemMedChem. 2007 Oct;2(10):1419-31. [Information]

[3]. Schuetz A, et al. Structural basis of inhibition of the human NAD-dependent deacetylase SIRT5 by suramin. Structure. 2007 Mar;15(3):377-89. [Information]

[4]. De Clercq E, et al. Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses. Cancer Lett. 1979 Nov;8(1):9-22. [Information]

[5]. Wanchao Yin, et al. Structural basis for inhibition of the SARS-CoV-2 RNA polymerase by suramin. Nat Struct Mol Biol. 2021 Mar;28(3):319-325. [Information]

[6]. Jindal HK, et al. Suramin affects DNA synthesis in HeLa cells by inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7. [Information]

[7]. Xiaozhe Zhang, et al. Suramin and NF449 Are IP5K Inhibitors That Disrupt IP6-mediated Regulation of Cullin RING Ligase and Sensitize Cancer Cells to MLN4924/pevonedistat. J Biol Chem. 2020 Jun 3;jbc.RA120.014375. [Information]

[8]. Novaes RD, et al. Purinergic Antagonist Suramin Aggravates Myocarditis and Increases Mortality by EnhancingParasitism, Inflammation, and Reactive Tissue Damage in Trypanosoma cruzi-Infected Mice. Oxid Med Cell Longev. 2018 Sep 30;2018:7385639. [Information]

[9]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Suramin hexasodium salt

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