| Chemical Properties | Back Directory | [Boiling point ]
636.068±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.331±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
4.390±0.40(predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
Endo CNTinh-03 is inhibitor for the elevation of cAMP and cGMP induced by agonist, such as G protein-coupled receptors, adenylate cyclase, and guanylate cyclase (IC50 is 4 μM). Endo CNTinh-03 inhibits cholera toxin- and Escherichia coli (STa) toxin- induced CFTR chloride current, ameliorates secretory diarrhea in mouse models, and prevents cyst growth in polycystic kidney disease model[1]. | [Biological Activity]
Cyclic nucleotide suppressor.
CNTinh-03 is a small-molecule general suppressors of cellular cyclic nucleotides. It reduces basal and agonist-induced elevation of cytoplasmic cAMP and cGMP in multiple cells and in response to different types of agonists. The mechanism of action involves nonselective activation of phosphodiesterase (PDE). | [References]
[1] Tradtrantip L, et al., Thiophenecarboxylate suppressor of cyclic nucleotides discovered in a small-molecule screen blocks toxin-induced intestinal fluid secretion. Mol Pharmacol. 2009 Jan;75(1):134-42. DOI:10.1124/mol.108.050567 |
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