| Identification | Back Directory | [Name]
Endovion | [CAS]
265646-85-3 | [Synonyms]
NS3728
Endovion
NS3728 >=98% (HPLC)
Urea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-[4-bromo-2-(2H-tetrazol-5-yl)phenyl]- | [Molecular Formula]
C16H9BrF6N6O | [MDL Number]
MFCD28147607 | [MOL File]
265646-85-3.mol | [Molecular Weight]
495.18 |
| Chemical Properties | Back Directory | [density ]
1.791±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 100 mM in DMSO and to 50 mM in ethanol | [form ]
Solid | [pka]
3.95±0.10(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water : < 0.1 mg/mL (insoluble) | [InChI]
1S/C16H9BrF6N6O/c17-9-1-2-11(13-26-28-29-27-13)12(6-9)25-14(30)24-10-4-7(15(18,19)20)3-8(5-10)16(21,22)23/h1-6H,(H2,24,25,30)(H,26,27,28,29) | [InChIKey]
OQRAKHDEGGGWQO-UHFFFAOYSA-N | [SMILES]
FC(F)(F)c1cc(cc(c1)C(F)(F)F)NC(=O)Nc2c(ccc(c2)Br)c3n[nH]nn3 |
| Hazard Information | Back Directory | [Biological Activity]
Endovion (NS3728) is an anion channel inhibitor (eg chloride channel) and a specific VRAC/VSOAC blocker. | [in vitro]
Endovion (NS3728, 10-100 μM) reduces TNFα-induced apoptosis and increases p53-protein level as well as downstream signaling, eg, expression of p21 Waf1/Cip1 , Bax, Noxa, MDM2, and activation of Caspase-9/-3 in Cisplatin-sensitive cells.
Endovion (NS3728, 10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines.
Western Blot Analysis | Cell Line: | Wild -type, resistant, and transiently transfected A2780 cells. | | Concentration: | 10-100 μM. < /td> | | Incubation Time: | 18 or 4.5 h. | < td class="col1"> Result: Reduced the maximal taurine rate constant more than 90% compared with the untreated control cells.
Resulted i n an increased LRRC8A protein expression.
Significantly reduced p53 and p21Waf1/Cip1 protein level in A2780WT cells.
| Cell Proliferation Assay | Cell Line: | Capan-1, AsPC-1, BxPC-3 and H6c7 cell lines. | | Concentration: | 10 μM. | | Incubation Time: | 24 h. | | Result: | Resulted in the most pronounced inhibition in all cell lines with 77 ± 26 % in Capan-1, 67 ± 9 % in AsPC-1, and 54 ± 8 % in BxPC-3 cells at +67 mV. | | [target]
Chloride channel, VRAC/VSOAC.
ANO1. | [storage]
Store at -20°C |
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