S0859
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MedKoo CAT#: 522671

CAS#: 1019331-10-2

Description: S0859 is a selective, high-affinity generic NBC inhibitor, potentially important for probing the transporter's functional role in heart and other tissues. S0859 reversibly inhibited NBC-mediated pH(i) recovery (K (i)=1.7 microM, full inhibition at approximately 30 microM). In HEPES-buffered superfusates, NHE-mediated pH(i) recovery was unaffected by 30 microM S0859. With CO(2)/HCO(3) (-) buffer, pH(i) recovery from intracellular alkalosis (mediated by Cl(-)/HCO(3) (-) and Cl(-)/OH(-) exchange) was also unaffected. .


Price and Availability

Size
Price

100mg
USD 1350
1g
USD 3750
Size
Price

200mg
USD 2150
2g
USD 5250
Size
Price

500mg
USD 2950
5g
USD 8950

S0859, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522671
Name: S0859
CAS#: 1019331-10-2
Chemical Formula: C29H24ClN3O3S
Exact Mass: 529.1227
Molecular Weight: 530.039
Elemental Analysis: C, 65.72; H, 4.56; Cl, 6.69; N, 7.93; O, 9.06; S, 6.05


Synonym: S0859; S-0859; S 0859.

IUPAC/Chemical Name: 2-chloro-N-((2'-(N-cyanosulfamoyl)-[1,1'-biphenyl]-4-yl)methyl)-N-(4-methylbenzyl)benzamide

InChi Key: ITDBPOSLOROLMT-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: O=C(N(CC1=CC=C(C2=CC=CC=C2S(=O)(NC#N)=O)C=C1)CC3=CC=C(C)C=C3)C4=CC=CC=C4Cl


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Heidtmann H, Ruminot I, Becker HM, Deitmer JW. Inhibition of monocarboxylate transporter by N-cyanosulphonamide S0859. Eur J Pharmacol. 2015 Sep 5;762:344-9. doi: 10.1016/j.ejphar.2015.05.049. Epub 2015 May 28. PubMed PMID: 26027796.

2: Fantinelli JC, Orlowski A, Aiello EA, Mosca SM. The electrogenic cardiac sodium bicarbonate co-transporter (NBCe1) contributes to the reperfusion injury. Cardiovasc Pathol. 2014 Jul-Aug;23(4):224-30. doi: 10.1016/j.carpath.2014.03.003. Epub 2014 Mar 19. PubMed PMID: 24721237.

3: Giambelluca MS, Ciancio MC, Orlowski A, Gende OA, Pouliot M, Aiello EA. Characterization of the Na/HCO3(-) cotransport in human neutrophils. Cell Physiol Biochem. 2014;33(4):982-90. doi: 10.1159/000358669. Epub 2014 Apr 1. PubMed PMID: 24714077.

4: Orlowski A, Vargas LA, Aiello EA, Álvarez BV. Elevated carbon dioxide upregulates NBCn1 Na+/HCO3(-) cotransporter in human embryonic kidney cells. Am J Physiol Renal Physiol. 2013 Dec 15;305(12):F1765-74. doi: 10.1152/ajprenal.00096.2013. Epub 2013 Sep 4. PubMed PMID: 24005470.

5: Larsen AM, Krogsgaard-Larsen N, Lauritzen G, Olesen CW, Honoré Hansen S, Boedtkjer E, Pedersen SF, Bunch L. 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. doi: 10.1002/cmdc.201200335. Epub 2012 Aug 27. PubMed PMID: 22927258.

6: Lauritzen G, Stock CM, Lemaire J, Lund SF, Jensen MF, Damsgaard B, Petersen KS, Wiwel M, Rønnov-Jessen L, Schwab A, Pedersen SF. 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. doi: 10.1016/j.canlet.2011.11.023. Epub 2011 Nov 25. PubMed PMID: 22120673.

7: Kumar S, Flacke JP, Kostin S, Appukuttan A, Reusch HP, Ladilov Y. SLC4A7 sodium bicarbonate co-transporter controls mitochondrial apoptosis in ischaemic coronary endothelial cells. Cardiovasc Res. 2011 Feb 1;89(2):392-400. doi: 10.1093/cvr/cvq330. Epub 2010 Oct 20. PubMed PMID: 20962104.

8: De Giusti VC, Orlowski A, Aiello EA. Angiotensin II inhibits the electrogenic Na+/HCO3- cotransport of cat cardiac myocytes. J Mol Cell Cardiol. 2010 Nov;49(5):812-8. doi: 10.1016/j.yjmcc.2010.07.018. Epub 2010 Aug 6. PubMed PMID: 20692267.

9: Ch'en FF, Villafuerte FC, Swietach P, Cobden PM, Vaughan-Jones RD. S0859, an N-cyanosulphonamide inhibitor of sodium-bicarbonate cotransport in the heart. Br J Pharmacol. 2008 Mar;153(5):972-82. doi: 10.1038/sj.bjp.0707667. Epub 2008 Jan 21. PubMed PMID: 18204485; PubMed Central PMCID: PMC2267275.

10: Avkiran M. Blowing off acid: a new tool to study Na+/HCO3- co-transport. Br J Pharmacol. 2008 Mar;153(5):844-5. doi: 10.1038/sj.bjp.0707670. Epub 2008 Jan 21. PubMed PMID: 18204484; PubMed Central PMCID: PMC2267277.

11: Yamamoto T, Swietach P, Rossini A, Loh SH, Vaughan-Jones RD, Spitzer KW. Functional diversity of electrogenic Na+-HCO3- cotransport in ventricular myocytes from rat, rabbit and guinea pig. J Physiol. 2005 Jan 15;562(Pt 2):455-75. Epub 2004 Nov 18. PubMed PMID: 15550467; PubMed Central PMCID: PMC1665517.