MilliporeSigma™ Calbiochem™ GIRK Activator, ML297

A blood-brain barrier-permeable, non-toxic phenyl-pyrazolylurea compound that acts as a direct, potent, fast, and reversible activator of GIRK1 (G-protein activated inward-rectifying K⁺ channel containing subunit 1) containing channels (EC₅₀ = 162, 914, and 887nM in Thallium influx assay for GIRK1/2, GIRK1/3, and GIRK1/4 expressed in HEK-293 cell

Supplier:  MilliporeSigma™ 5.05820.0001

Catalog No. 50-582-00001

Description

A blood-brain barrier-permeable, non-toxic phenyl-pyrazolylurea compound that acts as a direct, potent, fast, and reversible activator of GIRK1 (G-protein activated inward-rectifying K⁺ channel containing subunit 1) containing channels (EC₅₀ = 162, 914, and 887nM in Thallium influx assay for GIRK1/2, GIRK1/3, and GIRK1/4 expressed in HEK-293 cell lines). Its action does not require the presence of an activated G_i GPCR. Shown to be inactive towards GIRK2, GIRK2/3, K_ir2.1, K_V7.4 and GABA_A, and weakly active against a panel of 61 other receptors, ion channels, enzymes, transporters, and proteins even at higher concentration (∽10μM). Exhibits desirable pharmacokinetic properties with good solubility (17.5μM), predicted hepatic clearance (88 ml/min/kg), and T_max of 640nM and 130nM in plasma and brain, respectively. Shown to reduce locomotor function and seizure frequency in electroshock- and chemically-induced murine epilepsy models (60mg/kg, i.p).

Specifications

• Form: Powder
• Quantity: 10 mg
• Description: 98% by HPLC
• Molecular Formula: C₁₇H₁₄F₂N₄O

• Content And Storage: Protect from light
• Color: White
• Target Proteins: GIRK1/Kir3.1-containing tetrameric GIRK channels
• Solubility: DMSO