Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 31.00 | |
5 mg | In stock | $ 72.00 | |
10 mg | In stock | $ 122.00 | |
25 mg | In stock | $ 272.00 | |
50 mg | In stock | $ 438.00 | |
100 mg | In stock | $ 649.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 79.00 |
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. |
Targets&IC50 | KCC2:61 nM |
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[ |
Synonyms | N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide |
Molecular Weight | 382.5 |
Formula | C19H18N4OS2 |
CAS No. | 1391737-01-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/mL (52.29 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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VU0463271 1391737-01-1 Membrane transporter/Ion channel Potassium Channel Inhibitor KcsA VU-0463271 VU 0463271 inhibit N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide inhibitor