[CAS NO. 1019331-10-2] S0859

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Catalog:	HY-15529
Brand:	MCE
CAS:	1019331-10-2

Overview

MDL	MFCD23136018
Molecular Weight	530.04
Molecular Formula	C29H24ClN3O3S
SMILES	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

For research use only. We do not sell to patients.

Summary

S0859 is a selective, high-affinity generic Na ⁺ /HCO ₃ ^- transporter ( NBC ) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (K _i =1.7 μM, full inhibition at approximately 30 μM).

IC50 & Target

NBC ^[1]

In Vitro

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL ( 188.67 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.72 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

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