VU 0240551

SKU: orb1296176

Description

VU 0240551 is a selective, small-molecule antagonist of the neuronal K-Cl cotransporter KCC2, exhibiting an IC50 of 560 nM. It also demonstrates off-target activity by inhibiting L-type calcium channels and the hERG potassium channel. This compound is utilized in neuroscience research to investigate GABAergic signaling, neuronal excitability, and related pathophysiology in both cellular and animal models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 893990-34-6
• MW: 342.44
• Purity: 99.90%
• Formula: C₁₆H₁₄N₄OS₂
• SMILES: S(CC(NC=1SC=C(C)N1)=O)C2=CC=C(N=N2)C3=CC=CC=C3
• Target: Calcium Channel,Potassium Channel
• Solubility: H2O:Insoluble;DMSO:45 mg/mL (131.41 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.84 mM)

Bioactivity

• Target IC50:
  KCC2:560 nM
• In Vivo:
  VU 0240551 (10 μM) significantly inhibits chloride influx in cells from euhydrated rats, but does not affect cells from salt-loaded rats.
• In Vitro:
  VU 0240551 (0-100 μM) reduces the P cell response to GABA in a concentration-dependent manner and significantly reduces GABA-elicited hyperpolarization at doses of 75 and 100 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

hERG, L-type calcium channel, KCC2, Calcium Channel, CalciumChannel, PotassiumChannel, Potassium Channel, VU0240551, VU-0240551, VU 0240551

Compound Identifiers

PubChem CID

7211972