| Name | VU0463271 |
| Description | VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) is a potent and selective antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels, and transporters. |
| In vitro | VU0463271 is also found rapidly cleared in vitro[1]. VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively[2]. |
| In vivo | VU0463271(1 mg/kg; i.v.) is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg). The low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo[ |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 3.83 mg/mL (10.01 mM), Sonication is recommended.
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| Keywords | VU-0463271 | VU0463271 | VU 0463271 | PotassiumChannel | Potassium Channel | KcsA | KCC2 | Inhibitor | inhibit |
| Inhibitors Related | Minoxidil sulfate | Tannic acid | Hydrochlorothiazide | 1,8-Cineole | Tetraethylammonium bromide | Ursodeoxycholic acid | Chenodeoxycholic acid | Minoxidil | Chlorzoxazone | 2,2,2-Trichloroethanol | Taurocholic acid sodium salt hydrate | Indapamide |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
