S0859


CAS No. : 1019331-10-2

S0859,1019331-10-2
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000140
Synonyms:2-chloro-N-((2/'-(N-cyanosulfamoyl)-[1,1/'-biphenyl]-4-yl)methyl)-N-(4-methylbenzyl)benzamide
Molecular Formula:C₂₉H₂₄ClN₃O₃S
Molecular Weight:530.04
Target:Sodium Channel
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Appearance:Solid powder
Purity: > 98%
Cat No:I000140
Cas No:1019331-10-2
Product-Name:S0859
InChI:InChI=1S/C29H24ClN3O3S/c1-21-10-12-22(13-11-21)18-33(29(34)26-7-2-4-8-27(26)30)19-23-14-16-24(17-15-23)25-6-3-5-9-28(25)37(35,36)32-20-31/h2-17,32H,18-19H2,1H3
InChIKey:ITDBPOSLOROLMT-UHFFFAOYSA-N
SMILES:CC1=CC=C(C=C1)CN(CC2=CC=C(C=C2)C3=CC=CC=C3S(=O)(=O)NC#N)C(=O)C4=CC=CC=C4Cl

S0859, an N-cyanosulphonamide compound, reversibly inhibit NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM).
IC50 value:
Target: NBC
Na(+)-coupled HCO(3)(-) transporters (NBCs) mediate the transport of bicarbonate ions across cell membranes and are thus ubiquitous regulators of intracellular pH. NBC dysregulation is associated with a range of diseases; for instance, NBCn1 is strongly up-regulated in a model of ErbB2-dependent breast cancer, a malignant and widespread cancer with no targeted treatment options, and single-nucleotide polymorphisms in NBCn1 genetically link to breast cancer development and hypertension. Treatment with NBC inhibitor S0859 significantly increased caspase-3 activity and elevated the number of apoptotic EC. S0859 is potentially important for probing the transporter/'s functional role in heart and other tissues.


1:Inhibition of monocarboxylate transporter by N-cyanosulphonamide S0859. Heidtmann H, Ruminot I, Becker HM, Deitmer JW.Eur J Pharmacol. 2015 Sep 5;762:344-9. doi: 10.1016/j.ejphar.2015.05.049. Epub 2015 May 28. PMID: 26027796
2:Gram-scale solution-phase synthesis of selective sodium bicarbonate co-transport inhibitor S0859: in vitro efficacy studies in breast cancer cells. Larsen AM, Krogsgaard-Larsen N, Lauritzen G, Olesen CW, Honoré Hansen S, Boedtkjer E, Pedersen SF, Bunch L.ChemMedChem. 2012 Oct;7(10):1808-14. doi: 10.1002/cmdc.201200335. Epub 2012 Aug 27. PMID: 22927258
3:S0859, an N-cyanosulphonamide inhibitor of sodium-bicarbonate cotransport in the heart. Ch/'en FF, Villafuerte FC, Swietach P, Cobden PM, Vaughan-Jones RD.Br J Pharmacol. 2008 Mar;153(5):972-82. doi: 10.1038/sj.bjp.0707667. Epub 2008 Jan 21. PMID: 18204485 Free PMC Article
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