GSK2193874

SKU: orb1301628

Description

GSK2193874 is a potent and selective orally bioavailable TRPV4 channel antagonist. It is utilized in research to investigate TRPV4's role in pulmonary edema, neuropathic pain, and skeletal disorders, employing both in vitro cellular assays and in vivo animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1336960-13-4
• MW: 691.62
• Purity: 99.99%
• Formula: C₃₇H₃₈BrF₃N₄O
• SMILES: FC(F)(F)c1cccc(c1)-c1nc2cc(Br)ccc2c(C(=O)NC2(CC2)c2ccccc2)c1CN1CCC(CC1)N1CCCCC1
• Target: TRP/TRPV Channel
• Solubility: DMSO:81.67 mg/mL (118.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (5.78 mM)

Bioactivity

• Target IC50:
  TRPV4 (rat):2 nM (IC50)|TRPV4 (human):40 nM (IC50)
• In Vivo:
  In isolated rodent and canine lungs, TRPV4 blockade prevented the increased vascular permeability and resultant pulmonary edema associated with elevated PVP. In both acute and chronic HF models, GSK2193874 pretreatment inhibited the formation of pulmonary edema and enhanced arterial oxygenation.
• In Vitro:
  GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents[1,2].
• Animal Research:
  Adult male Sprague-Dawley rats (n = 7 to 8 per group) were treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg/day) via oral gavage for at least 4 days before osmotic challenges. Rats underwent acute and chronic hyper- and hypo-osmotic challenges.Sprague-Dawley (control, n = 18) and spontaneously hypertensive rats (n = 11) were implanted with Data Sciences International (DSI) radiotelemetry transmitters. Rats were dosed with GSK2193874, and data were captured with DSI receivers and analyzed with Microsoft Excel.

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

inhibit, Inhibitor, GSK 2193874, GSK2193874, GSK-2193874, TRP Channel, TRPChannel, TRPV Channel, TRPV4, TRPVChannel, Transient receptor potential channels

Compound Identifiers

PubChem CID

53464483