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S0859

Catalog No.GC10615

A selective sodium/bicarbonate cotransporter blocker

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S0859 Chemical Structure

Cas No.: 1019331-10-2

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5mg
$59.00
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10mg
$99.00
In stock
50mg
$396.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Description of S0859

S0859 is a selective, high-affinity generic 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].

References:
[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.

Chemical Properties of S0859

Cas No. 1019331-10-2 SDF
Chemical Name 2-chloro-N-((2'-(N-cyanosulfamoyl)-[1,1'-biphenyl]-4-yl)methyl)-N-(4-methylbenzyl)benzamide
Canonical SMILES CC1=CC=C(CN(C(C2=CC=CC=C2Cl)=O)CC3=CC=C(C4=CC=CC=C4S(=O)(NC#N)=O)C=C3)C=C1
Formula C29H24ClN3O3S M.Wt 530.04
Solubility DMF: 50 mg/mL,DMSO: 30 mg/mL,Ethanol: 50 mg/mL,PBS (pH 7.2): 10 mg/mL Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of S0859

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1 mg 5 mg 10 mg
1 mM 1.8867 mL 9.4333 mL 18.8665 mL
5 mM 0.3773 mL 1.8867 mL 3.7733 mL
10 mM 0.1887 mL 0.9433 mL 1.8867 mL
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In vivo Formulation Calculator (Clear solution) of S0859

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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