Bioactivity | 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). | ||||||||||||
Target | NBC | ||||||||||||
Invitro | 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]. | ||||||||||||
Name | S0859 | ||||||||||||
CAS | 1019331-10-2 | ||||||||||||
Formula | C29H24ClN3O3S | ||||||||||||
Molar Mass | 530.04 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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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. |