For research use only. Not for therapeutic Use.
S0859 is a selective, high-affinity generic Na+/HCO3- transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
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].
| Catalog Number | I000140 |
| CAS Number | 1019331-10-2 |
| Synonyms | 2-chloro-N-[[4-[2-(cyanosulfamoyl)phenyl]phenyl]methyl]-N-[(4-methylphenyl)methyl]benzamide |
| Molecular Formula | C29H24ClN3O3S |
| Purity | ≥95% |
| 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 |
| Reference | [1]. Larsen AM, Krogsgaard-Larsen N, Lauritzen G, et al. Gram-scale solution-phase synthesis of selective sodium bicarbonate co-transport inhibitor S0859: in vitro efficacy studies in breast cancer cells. ChemMedChem. 2012 Oct;7(10):1808-14. [2]. Lauritzen G, Stock CM, Lemaire J, et al. The Na+/H+ exchanger NHE1, but not the Na+, HCO3(-) cotransporter NBCn1, regulates motility of MCF7 breast cancer cells expressing constitutively active ErbB2. Cancer Lett. 2012 Apr 28;317(2):172-83. [3]. Kumar S, Flacke JP, Kostin S, et al. SLC4A7 sodium bicarbonate co-transporter controls mitochondrial apoptosis in ischaemic coronary endothelial cells. Cardiovasc Res. 2011 Feb 1;89(2):392-400. [4]. Ch’en FF, Villafuerte FC, Swietach P, et al. S0859, an N-cyanosulphonamide inhibitor of sodium-bicarbonate cotransport in the heart. Br J Pharmacol. 2008 Mar;153(5):972-82. |
