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Submit ReviewSuramin hexasodium salt is a non-selective P2 purinergic antagonist. Also blocks calmodulin binding to recognition sites and G protein coupling to G protein-coupled receptors. Increases open probability of ryanodine receptor (RyR) channels and acts as a competitive α1β2γ2 GABAA receptor antagonist. Anticancer, antiviral and antiparasitic agent.
This product may be supplied with a high degree of hydration and some residual NaCl, the amounts of which are batch dependent. Please refer to the Certificate of Analysis to obtain the batch specific Net Product Content.
M. Wt | 1429.15 |
Formula | C51H34N6Na6O23S6 |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 129-46-4 |
PubChem ID | 5360 |
InChI Key | VAPNKLKDKUDFHK-UHFFFAOYSA-H |
Smiles | [Na+].[Na+].[Na+].[Na+].[Na+].[Na+].CC1=CC=C(C=C1NC(=O)C1=CC=CC(NC(=O)NC2=CC=CC(=C2)C(=O)NC2=C(C)C=CC(=C2)C(=O)NC2=C3C(C=C(C=C3S([O-])(=O)=O)S([O-])(=O)=O)=C(C=C2)S([O-])(=O)=O)=C1)C(=O)NC1=C2C(C=C(C=C2S([O-])(=O)=O)S([O-])(=O)=O)=C(C=C1)S([O-])(=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 50 | 35 | |
DMSO | 5 | 4 |
The following data is based on the product molecular weight 1429.15. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.35 mM | 2 mL | 10 mL | 19.99 mL |
1.75 mM | 0.4 mL | 2 mL | 4 mL |
3.5 mM | 0.2 mL | 1 mL | 2 mL |
17.5 mM | 0.04 mL | 0.2 mL | 0.4 mL |
References are publications that support the biological activity of the product.
Beindl et al (1996) Inhibition of receptor/G protein coupling by suramin analogues. Mol.Pharmacol. 50 415 PMID: 8700151
Charlton et al (1996) PPADS and suramin as antagonists at cloned P2Y- and P2U-purinoceptors. Br.J.Pharmacol. 118 704 PMID: 8762097
Klinger et al (2001) Suramin and the suramin analogue NF307 discriminate among calmodulin-binding sites. Biochem.J. 355 827 PMID: 11311147
Voogd et al (1993) Recent research on the biological activity of suramin. Pharmacol.Rev. 45 177 PMID: 8396782
Hill et al (2004) Functional regulation of the cardiac ryanodine receptor by suramin and calmodulin involves multiple binding sites. Mol.Pharmacol. 65 1258 PMID: 15102954
Luo et al (2018) Suramin is a novel competitive antagonist selective to α1β2γ2 GABAA over ρ1 GABAC receptors. Neuropharmacology. 141 148 PMID: 30172846
If you know of a relevant reference for Suramin hexasodium salt, please let us know.
Keywords: Suramin hexasodium salt, Suramin hexasodium salt supplier, Non-Selective, P2, antagonists, P2X, P2Y, Uncouples, G, proteins, from, receptors, heterotrimeric, purinoceptors, ryanodine, ion, channels, GABAA, antagonism, Receptors, Heterotrimeric, G-protein, GTPases, Purinergic, Ryanodine, 1472, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Suramin hexasodium salt include:
Naviaux et al (2015) Antipurinergic therapy corrects the autism-like features in the Fragile X (Fmr1 knockout) mouse model. Mol Autism 6 1 PMID: 25705365
Fonseca et al (2015) Diadenosine tetraphosphate contributes to CB-induced tear secretion. Purinergic Signal 11 87 PMID: 25398705
Tang et al (2015) Stimulation-evoked Ca2+ signals in astrocytic processes at hippocampal CA3-CA1 synapses of adult mice are modulated by glutamate and ATP. J Neurosci 35 3016 PMID: 25698739
Thrane et al (2011) Critical role of aquaporin-4 (AQP4) in astrocytic Ca2+ signaling events elicited by cerebral edema. Proc Natl Acad Sci U S A 108 846 PMID: 21187412
Dosch et al (2019) Connexin-43-dependent ATP release mediates macrophage activation during sepsis. Elife 8 PMID: 30735126
Conley (2017) Imaging extracellular ATP with a genetically-encoded, ratiometric fluorescent sensor. PLoS One 12 e0187481 PMID: 29121644
Naviaux et al (2013) Antipurinergic therapy corrects the autism-like features in the poly(IC) mouse model. PLoS One 8 e57380 PMID: 23516405
Zierhut (2017) Role of purinergic signaling in experimental pneumococcal meningitis. Sci Rep 7 44625 PMID: 28300164
Nishimura et al (2015) The Suramin Derivative NF449 Interacts with the 5-fold Vertex of the Enterovirus A71 Capsid to Prevent Virus Attachment to PSGL-1 and Heparan Sulfate. PLoS Pathog 11 e1005184 PMID: 26430888
Makris et al (2015) Digoxin and adenosine triphosphate enhance the functional properties of tissue-engineered cartilage. Tissue Eng Part A 21 884 PMID: 25473799
Sivaramakrishnan et al (2012) Constitutive lysosome exocytosis releases ATP and engages P2Y receptors in human monocytes. J Cell Sci 125 4567 PMID: 22767503
Yuryev et al (2016) In vivo Calcium Imaging of Evoked Calcium Waves in the Embryonic Cortex. Front Cell Neurosci 9 500 PMID: 26778965
Rosa et al (2015) Neuron-glia signaling in developing retina mediated by neurotransmitter spillover. J Mol Neurosci 4 PMID: 26274565
Ibáñez et al (2012) A high throughput scintillation proximity imaging assay for protein methyltransferases. Comb Chem High Throughput Screen 15 359 PMID: 22256970
Hazleton et al (2012) Purinergic receptors are required for HIV-1 infection of primary human macrophages. J Immunol 188 4488 PMID: 22450808
Manohar et al (2012) ATP release and autocrine signaling through P2X4 receptors regulate γδ T cell activation. J Leukoc Biol 92 787 PMID: 22753954
Ledderose et al (2016) Mitochondrial Dysfunction, Depleted Purinergic Signaling, and Defective T Cell Vigilance and Immune Defense. J Infect Dis 213 456 PMID: 26150546
Zhang et al (2016) Signaling mechanism for modulation by ATP of glycine receptors on rat retinal ganglion cells. Sci Rep 6 28938 PMID: 27357477
Rodríguez-Zayas et al (2012) Blockade of P2 nucleotide receptors after spinal cord injury reduced the gliotic response and spared tissue. Am J Physiol Heart Circ Physiol 46 167 PMID: 21647706
Mikolajewicz et al (2018) Mechanically stimulated ATP release from murine bone cells is regulated by a balance of injury and repair. Elife 7 PMID: 30324907
Naviaux et al (2014) Reversal of autism-like behaviors and metabolism in adult mice with single-dose antipurinergic therapy. Transl Psychiatry 4 e400 PMID: 24937094
Malmersjö et al (2013) Neural progenitors organize in small-world networks to promote cell proliferation. J Pharmacol Exp Ther 110 E1524 PMID: 23576737
Verma et al (2005) Modulation of agonist binding to human DA receptor subtypes by L-prolyl-L-leucyl-glycinamide and a peptidomimetic analog. Elife 315 1228 PMID: 16126839
Price et al (2004) Cannabinoid receptor-independent actions of the aminoalkylindole WIN 55,212-2 on trigeminal sensory neurons. Br J Pharmacol 142 257 PMID: 15155534
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The ATP induced expression of p-LKB1 was inhibited by Suramin in Cancer Cells.
used to study synchronized calcium oscillations in co-cultures of neurons and glial cells
50 micromolar of suramin was bath applied
Non-specific P2X blocker, worked as expected.