S0859 | CAS#1019331-10-2

S0859
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WARNING: This product is for research use only, not for human or veterinary use.

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. .

Chemical Structure

S0859

CAS# 1019331-10-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 522671
Name: S0859
CAS#: 1019331-10-2
Chemical Formula: C29H24ClN3O3S
Exact Mass: 529.12
Molecular Weight: 530.040
Elemental Analysis: C, 65.72; H, 4.56; Cl, 6.69; N, 7.93; O, 9.06; S, 6.05

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 450	2 Weeks
50mg	USD 900	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

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: To be determined

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).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	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.
In vitro activity:	This study describes an efficient method to synthesize S0859 and investigated its inhibitory effect on intracellular pH recovery after an acid load was confirmed in human and murine cancer cell lines. S0859 exhibited strong binding to plasma components, rendering it ineffective in isolated murine tissues at concentrations up to 50 μM Reference: ChemMedChem. 2012 Oct;7(10):1808-14. https://pubmed.ncbi.nlm.nih.gov/22927258/
In vivo activity:	This study found that ischemiareperfusion increased Na+ coupled HCO3-transporters’ current, inhibited the excitability of hippocampal CA1 neurons, and led to apoptosis in CA1 neurons. S0859 protected CA1 neurons from ischemiareperfusion induced neuronal cell death, astrocyte accumulation, and spatial memory impairment. These findings indicate that S0859 could be a promising target to protect neuronal functions after ischemiareperfusion. Reference: CNS Neurol Disord Drug Targets. 2023;22(7):1109-1119. https://pubmed.ncbi.nlm.nih.gov/35585807/

Preparing Stock Solutions

The following data is based on the product molecular weight 530.04 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
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. 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. PMID: 24005470. 2. 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. PMID: 22927258. 3. Jia M, Zhang Q, Guo X, Liu R, Liu S, Chen N, Wang Y, Wang Q, Wu J, Campbell SL. Na+/HCO3- Co-transporters Inhibitor S0859 Attenuates Global Cerebral Ischemia-reperfusion Injury of the CA1 Neurons in the Gerbil's Hippocampus. CNS Neurol Disord Drug Targets. 2023;22(7):1109-1119. doi: 10.2174/1871527321666220517121135. PMID: 35585807. 4. Ji M, Ryu HJ, Baek HM, Shin DM, Hong JH. Dynamic synovial fibroblasts are modulated by NBCn1 as a potential target in rheumatoid arthritis. Exp Mol Med. 2022 Apr;54(4):503-517. doi: 10.1038/s12276-022-00756-6. Epub 2022 Apr 12. PMID: 35414711; PMCID: PMC9076869.
In vitro protocol:	1. 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. PMID: 24005470. 2. 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. PMID: 22927258.
In vivo protocol:	1. Jia M, Zhang Q, Guo X, Liu R, Liu S, Chen N, Wang Y, Wang Q, Wu J, Campbell SL. Na+/HCO3- Co-transporters Inhibitor S0859 Attenuates Global Cerebral Ischemia-reperfusion Injury of the CA1 Neurons in the Gerbil's Hippocampus. CNS Neurol Disord Drug Targets. 2023;22(7):1109-1119. doi: 10.2174/1871527321666220517121135. PMID: 35585807. 2. Ji M, Ryu HJ, Baek HM, Shin DM, Hong JH. Dynamic synovial fibroblasts are modulated by NBCn1 as a potential target in rheumatoid arthritis. Exp Mol Med. 2022 Apr;54(4):503-517. doi: 10.1038/s12276-022-00756-6. Epub 2022 Apr 12. PMID: 35414711; PMCID: PMC9076869.

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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.

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