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Suramin hexasodium salt

目录号 GC16832

P2 purinergic antagonist

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,310.00
现货
25mg
¥2,100.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Kinase experiment:

The ATPase assay is performed in a 10 μL reaction mixture containing 20 mM Tris-HCl (pH 7.5), 1 mM DTT, 8 mM MgCl2, 5 μM M13 circular ssDNA, 2.5 μM RecA from the specified bacterial species and increasing concentrations of suramin. The reaction is initiated by the addition of 2 mM [α-32P]ATP, incubated for 30 min at 37°C and stopped by the addition of 25 mM EDTA[2].

Animal experiment:

Rats: To assess the potential preventive and curative effects of suramin, rats are randomly divided into four groups after MCT injection. In the preventive strategy, the treatment is started on the first day, and one group receives 10 mg/kg suramin intravenously twice weekly for 3 weeks, while a second group receives only the vehicle at the same time points. To assess the potential curative effects of suramin, rats are given MCT and are left untreated for 21 days before being randomly divided into two groups that are subsequently treated with either suramin or vehicle from day 21 to day 42 inclusive. The effect of suramin on survival is evaluated from the day 21 of MCT injection to day 42 corresponding to the treatment period[4].

References:

[1]. 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.
[2]. Nautiyal A, et al. Suramin is a potent and selective inhibitor of Mycobacterium tuberculosis RecA protein and the SOS response: RecA as a potential target for antibacterial drug discovery. J Antimicrob Chemother. 2014 Jul;69(7):1834-43.
[3]. Bojanowski K, et al. Suramin is an inhibitor of DNA topoisomerase II in vitro and in Chinese hamster fibrosarcomacells. Proc Natl Acad Sci U S A. 1992 Apr 1;89(7):3025-9.
[4]. Izikki M, et al. The beneficial effect of suramin on monocrotaline-induced pulmonary hypertension in rats. PLoS One. 2013 Oct 15;8(10):e77073.
[5]. J Biol Chem. 1999 Jul 2;274(27):18997-9002.Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5.

产品描述

Suramin is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM).[1],[2[ Suramin also acts as a non-specific competitor of glycosaminoglycan binding to a variety of targets including TGFβ, PDGF, and FGF and additionally inhibits insulin-like growth factor-l, EGF, PKC activity, TNF, IL-2, transferrin, and Apo-B.[3] While originally used as an early stage treatment of trypanosome-caused onchocerciasis (African river blindness) and African trypanosomiasis (African sleeping sickness), suramin has been under clinical evaluation for its potential to regress a number of cancer cell lines, including non-small cell lung cancer, advanced breast cancer, hormone refractory prostate cancer, metastatic renal cell cancer, colorectal cancer, and high-grade gliomas.[3],[4],[5]

Reference:

[1]. Klinger, M., Bofill-Cardona, E., Mayer, B., et al. Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sites Biochemistry Journal 355(3), 827-833 (2001).
[2]. Charlton, S.J., Brown, C.A., Weisman, G.A., et al. PPADS and suramin as antagonists at cloned P2Y- and P2U- purinoceptors British Journal of Pharmacology 118(3), 704-710 (1996).
[3]. Eisenberger, M.A., and Reyno, L.M. Suramin Cancer Treatment Reviews 20, 259-273 (1994).
[4]. Stein, C.A. Suramin: A novel antineoplastic agent with multiple potential mechanisms of action Cancer Research 53, 2239-2248 (1993).
[5]. McGeary, R.P., Bennett, A.J., Tran, Q.B., et al. Suramin: Clinical uses and structure-activity relationships Mini Rev.Med.Chem. 8(13), 1384-1394 (2008).

Chemical Properties

Cas No. 129-46-4 SDF
别名 N/A
化学名 sodium 8,8'-((3,3'-((3,3'-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(4-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,5-trisulfonate)
Canonical SMILES [O-]S(=O)(C1=C(C(NC(C2=CC=C(C)C(NC(C3=CC=CC(NC(NC4=CC(C(NC5=CC(C(NC(C(C6=CC(S([O-])(=O)=O)=C7)=C7S([O-])(=O)=O)=CC=C6S([O-])(=O)=O)=O)=CC=C5C)=O)=CC=C4)=O)=C3)=O)=C2)=O)=CC=C8S([O-])(=O)=O)C8=CC(S([O-])(=O)=O)=C1)=O.[Na+].[Na+].[Na+].[Na+].[Na+].[Na+]
分子式 C51H34N6Na6O23S6 分子量 1429.15
溶解度 ≥ 71.45mg/mL in H2O 储存条件 4°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

动物体内配方计算器 (澄清溶液)

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