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Chemical Structure| 1019331-10-2 Chemical Structure| 1019331-10-2

Structure of S0859
CAS No.: 1019331-10-2

Chemical Structure| 1019331-10-2

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S0859 is a selective, high-affinity inhibitor of Na+/HCO3- cotransporter (NBC), reversibly inhibiting NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, complete inhibition at 30 μM).

Synonyms: S0859

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Product Details of S0859

CAS No. :1019331-10-2
Formula : C29H24ClN3O3S
M.W : 530.04
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
Synonyms :
S0859
MDL No. :MFCD23136018

Safety of S0859

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 20 µM 24 hours To evaluate the effect of S0859 on cell migration, results showed that S0859 partially inhibited cell motility. Pharmaceutics. 2020 Aug 27;12(9):816
Mouse hippocampal neurons 50 µM 30 minutes To investigate the effect of S0859 on GABA A receptor-mediated postsynaptic currents. Results showed that S0859 completely inhibited postsynaptic GABA AR and, thus, could not be used as a tool to investigate the role of NBCs in GABA-dependent neuronal networks. Front Cell Neurosci. 2023 Oct 10;17:1253424
HEK-293 cells 50 µM 30 minutes To investigate the effect of NBC inhibitor S0859 on KCC2 activity. Results showed that S0859 prevented staurosporine- and 4-aminopyridine(4AP)-induced KCC2 activation. Front Cell Neurosci. 2023 Oct 10;17:1253424
Mouse renal afferent arterioles 50 µM 30 minutes S0859, an inhibitor of the NBC family, blocked the NaHCO3-induced increase in pH i and vasodilation Hypertension. 2019 Nov;74(5):1104-1112
LNCaP cells 50 µM 4 days To assess the role of NBCe1 in LNCaP cell proliferation and viability, results showed that S0859 treatment decreased the number of viable cells Oncol Rep. 2021 Jul;46(1):129
Ciliated human nasal epithelial cells (c-hNECs) 30 µM 5 minutes S0859 decreased the CBF ratio from 1.00 to 0.79, indicating that the NBC inhibitor reduced HCO3- influx, thereby lowering pH i and CBF. Int J Mol Sci. 2024 Aug 21;25(16):9069
PC3 cells 100 µM 6 days To assess the role of NBCe1 in PC3 cell proliferation and viability, results showed that S0859 treatment decreased the number of viable cells Oncol Rep. 2021 Jul;46(1):129
Human keratinocytes (HaCaT) 100 µM 6 hours To evaluate the inhibitory effect of S0859 on SLS-induced cytotoxicity in keratinocytes. Results showed that S0859 significantly inhibited SLS-dependent cell death. Front Cell Infect Microbiol. 2022 Nov 1;12:1002230
RA-FLSs (rheumatoid arthritis fibroblast-like synoviocytes) 20 µM 6 hours To evaluate the inhibitory effect of S0859 on RA-FLSs migration. Results showed that S0859 significantly reduced TNF-α or RA synovial fluid-stimulated RA-FLSs migration. Exp Mol Med. 2022 Apr;54(4):503-517
MCF-7 cells 50 µM 7 days To evaluate the effect of S0859 on MCF-7 spheroid growth, results showed that S0859 combined with MCT1 inhibitor AR-C155858 further reduced spheroid diameter Mol Cancer. 2016 Jun 6;15(1):45

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Necrotizing skin infection model Subcutaneous injection 200 µM Initial injection followed by additional doses at 4 and 8 hours post-infection, lasting 24 hours To evaluate the effect of S0859 on SLS-dependent skin lesions. Results showed that S0859 treatment did not significantly affect SLS-mediated skin lesion size. Front Cell Infect Microbiol. 2022 Nov 1;12:1002230
DBA/1 mice Collagen-induced arthritis (CIA) model Tail vein injection 800 ng/g Two injections, two weeks apart To evaluate the inhibitory effect of S0859 on joint swelling and destruction in the CIA mouse model. Results showed that S0859 reduced joint swelling and destruction without blood, hepatic, or renal toxicity. Exp Mol Med. 2022 Apr;54(4):503-517

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.43mL

1.89mL

0.94mL

18.87mL

3.77mL

1.89mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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