Suramin Hexasodium Salt
A sodium salt shape of suramin, a polysulphonated naphthylurea with cappotential antineoplastic activity. Suramin blocks the binding of numerous boom factors, which includes insulin-like boom thing I (IGF-I), epidermal boom thing (EGF), platelet-derived boom thing (PDGF), and tumor boom thing-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cellular proliferation and migration. This agent additionally inhibits vascular endothelial boom thing (VEGF)- and primary fibroblast boom thing (bfgf)-prompted angiogenesis; retroviral opposite transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cell folate transport; and steroidogenesis.
Background
Suramin Hexasodium Salt, as a polysulfonated naphthylurea, is a powerful aggressive inhibitor of DNA topoisomerase II, with an IC50 of five μm.
DNA topoisomerase II cuts each strands of the DNA helix concurrently to control DNA tangles and supercoils. Once reduce, the ends of the DNA are separated and every other DNA duplex surpassed thru the break. Then the reduce DNA is religated.
Suramin Hexasodium Salt can inhibit cellular proliferation and DNA synthesis in hela cells culture. It abolishes the replication of SV40 DNA absolutely with forty μm concentration. DNA polymerase α is extra touchy to concentrations of suramin than DNA polymerase δ with the IC50 of eight µm and 36 µm respectively. Suramin is a powerful inhibitor of DNA strand trade and atpase sports of bacterial reca proteins and reca-catalysed proteolytic cleavage of the lexa repressor. The inhibition mechanism of suramin includes its cappotential to disassemble reca–unmarried-stranded DNA filaments.
In the animal assay, in comparison to manipulate rats, remedy with suramin suggests decrease values for pulmonary artery pressure, proper ventricular hypertrophy, and distal vessel muscularization on day 21. Suramin remedy suppresses PA-SMC proliferation and attenuates each the inflammatory reaction and the deposition of collagen.
References:
[1].Jindal HK, et al. Suramin influences DNA synthesis in hela cells through inhibition of DNA polymerases. Cancer Res. 1990 Dec 15;50(24):7754-7.
[2].Nautiyal A, et al. Suramin is a powerful and selective inhibitor of Mycobacterium tuberculosis reca protein and the SOS reaction: reca as a cappotential goal 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 useful impact of suramin on monocrotaline-prompted pulmonary high blood pressure in rats. Plos One. 2013 Oct 15;eight(10):e77073.
Chemical Properties
· Physical Appearance A solid
· Storage Store at RT
· M.Wt 1429.15
· Cas No. 129-46-four
· Formula C51H34N6Na6O23S6
· Solubility ≥71.forty five mg/ml in H2O; insoluble in etoh; ≥21 mg/ml in DMSO
· Chemical Name sodium eight,eight’-((3,3′-((3,3′-(carbonylbis(azanediyl))bis(benzoyl))bis(azanediyl))bis(four-methylbenzoyl))bis(azanediyl))bis(naphthalene-1,3,five-trisulfonate)
General suggestions For acquiring a better solubility, please heat the tube at 37°C and shake it withinside the ultrasonic tubtub for a while. We do now no longer suggest long-time period garage for the solution, please use it up soon.
Buy Suramin Hexasodium Salt
A polyanionic compound with an unknown mechanism of action. It is used parenterally withinside the remedy of African trypanosomiasis and it’s been used clinically with diethylcarbamazine to kill the person Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has additionally been proven to have powerful antineoplastic properties.
A polyanionic compound with an unknown mechanism of action. It is used parenterally withinside the remedy of African trypanosomiasis and it’s been used clinically with diethylcarbamazine to kill the person Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has additionally been proven to have powerful antineoplastic properties. Suramin is synthetic through Bayer in Germany as Germanin. Also acknowledged as: Naphuride, Germanin, Naganol, Belganyl, Fourneau, Farma, Antrypol, Suramine, Naganin
· 8,8′-di(1,3,5-naphthalenetrisulfonic acid) …FREE FORM
· 8,8′-[Ureylenebis[m-phenylenecarbonylimino(4-methyl-m-phenylene)carbonylimino]]di(1,3,five-naphthalenetrisulfonic acid) hexasodium salt
· CAS 145-63-1 FREE FORM
· 129-46-four of hexa sodium
· LAUNCHED 1940 BAYER
The molecular formulation of suramin is C51H34N6O23S6. It is a symmetric molecule withinside the middle of which lies urea, NH-CO-NH. Suramin carries eightbenzene rings, 4 of which might be fused in pairs (naphthalene), 4 amide companies similarly to the only of urea and six sulfonate companies. When given as drug it generally carries six sodium ions that shape a salt with the six sulfonate companies.
Suramin Hexasodium Salt is a drug advanced through Oskar Dressel and Richard Kothe of Bayer, Germany in 1916, and remains offered through Bayer below the emblem namegermanin. Suramin sodium is a heparanase inhibitor that become first released in 1940 through Bayer below the emblem call Antrypol for the remedy of helminthic infection. It become later released through Bayer for the remedy of trypanosomiasis (African slumbering sickness). More recently, the product has entered early medical improvement at Ohio State University for the remedy of platinum-pretreated sufferers with degree IIIB/IV non-small cellular lung cancer, in mixture with docetaxel or gemcitabine. The National Cancer Institute (NCI) is carrying out section II medical research for the remedy of glioblastoma multiforme and for the remedy of adrenocortical carcinoma.
According to the National Cancer Institute there aren’t anyt any energetic medical trials (as of April 1, 2008). Completed and closed medical trials are indexed here:
· In addition to Germanin, the National Cancer Institute additionally lists the following “Foreign emblem names”: 309 F or 309 Fourneau, Bayer 205, Moranyl, Naganin, Naganine.
· Suramin is run through a unmarried weekly intravenous injection for 6 weeks. The dose in line with injection is 1 g.
· The maximum common detrimental reactions are nausea and vomiting. About 90% of sufferers gets an urticarial rash that disappears in some days with no need to prevent remedy. There is a extra than 50% risk of adrenal cortical harm, however handiest a smaller percentage would require lifelongcorticosteroid replacement. It is not unusualplace for sufferers to get a tingling or crawling sensation of the pores and skin with suramin. Suramin will reason clouding of the urine that’s harmless: sufferers ought to be warned of this to keep away from them turning into alarmed.
· Kidney harm and exfoliative dermatitis arise much less commonly.
· Suramin has been implemented clinically to HIV/AIDS sufferers ensuing in a big variety of deadly occurrences and as a end result the software of this molecule become deserted for this condition.
· Suramin is likewise utilized in studies as a broad-spectrum antagonist of P2 receptors and agonist of Ryanodine receptors.
· In addition to antagonism of P2 receptors, Suramin inhibits the acitivation of heterotrimeric G proteins in numerous different gpcrs with various potency. It prevents the affiliation of heteromeric G proteins and consequently the receptors Guanine trade functionality (GEF). With this blockade the GDP will now no longer launch from the Gα subunit so it cannot get replaced through a GTP and come to be activated. This has the impact of blocking off downstream G protein mediated signaling of numerous GPCR proteins which includes Rhodopsin, the A1 Adenosine receptor, and the D2 dopamine receptor.
· A polyanionic compound with an unknown mechanism of action. It is used parenterally withinside the remedy of African trypanosomiasis and it’s been used clinically with diethylcarbamazine to kill the person Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has additionally been proven to have powerful antineoplastic properties. Suramin is synthetic through Bayer in Germany as Germanin.