VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)

Cas No.:	1391737-01-1
Chemical Name:	(N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)
SMILES:	O=C(N(C1CC1)C2=NC(C)=CS2)CSC3=NN=C(C4=CC=CC=C4)C=C3
Formula:	C₁₉H₁₈N₄Os₂
M.Wt:	382.5
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

In Vitro VU0463271 is a potent 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. It is also found rapidly cleared in vitro. In Vivo VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/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.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC73605	TMinh-23	TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity).
DC73604	TMEM16A blocker 1PBC	1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).
DC73603	OV350	OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.
DC70312	CLC-2-IN-AK42	CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.AK-42 binds to an extracellular vestibule above the channel pore. AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.AK-42 is a powerful tool for investigating CLC-2 neurophysiology.
DC47321	Endovion (NS 3728)	Endovion (NS 3728, SCO-101) is an potent anion channel inhibitor that blocks the Volume Regulated Anion Channels (VRAC).
DC29060	Picrotoxinin	Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors.
DC12169	VU0463271	VU0463271 is a potent KCC2 antagonist, with an IC50 of 61 nM.
DC11173	DRAinh-A250	DRAinh-A250 is a specific inhibitor of Cl-/anion exchanger SLC26A3 (DRA), fully and reversibly inhibits SLC26A3-mediated Cl- exchange with HCO3-, I-, and thiocyanate (SCN-) with IC50 of ~0.2 uM.
DC11507	CLP257	CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport i
DC73606	VI-116	VI-116 is a potent and selective volume-regulated anion channel (VRAC) inhibitor, fully inhibits VRAC-mediated I- quenching with an IC50 of 1.27 uM in LN215 cells.