SML0942

GSK2193874

≥98% (HPLC), TRPV4 ion channel antagonist, powder

• Synonym(s): 3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
• Empirical Formula (Hill Notation): C₃₇H₃₈BrF₃N₄O
• CAS Number: 1336960-13-4
• Molecular Weight: 691.62
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Product Name: GSK2193874, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: >5 mg/mL, clear
• storage temp.: room temp
• SMILES string: FC(F)(F)c1cc(ccc1)c2nc3c(c(c2CN6CCC(CC6)N7CCCCC7)C(=O)NC5(CC5)c4ccccc4)ccc(c3)Br
• InChI: 1S/C37H38BrF3N4O/c38-28-12-13-30-32(23-28)42-34(25-8-7-11-27(22-25)37(39,40)41)31(24-44-20-14-29(15-21-44)45-18-5-2-6-19-45)33(30)35(46)43-36(16-17-36)26-9-3-1-4-10-26/h1,3-4,7-13,22-23,29H,2,5-6,14-21,24H2,(H,43,46)
• InChI key: UIVOZBSCHXCGPS-UHFFFAOYSA-N

Description

Application

GSK2193874 has been used as a transient receptor potential vanilloid 4 (TRPV4) antagonist:

• to study its effects on GSK101-induced colon contractions in mice[1]
• to study its effects on murine compact bone-derived osteoblasts(CB-OB)[2]
• to study its effects on lung injury post-lipopolysaccharide (LPS) in mice[3]

Biochem/physiol Actions

GSK2193874 is a very potent, specific antagonist of TRPV4 ion channels (IC₅₀ = 50 nM). Lung edema caused by high pulmonary venous pressure (PVP) is driven by TRPV4 activity. GSK2193874 blocks TRPV4-mediated calcium influx in cells expressing native and recombinant TRPV4, and inhibits vascular permeability and lung edema in isolated rodent and canine lungs subjected to high PVP. The compound also resolves pulmonary edema in murine myocardial infarction model.

GSK2193874 is a very potent, specific antagonist of TRPV4.

Safety Information

• pictograms: GHS06
• signalword: Danger
• hcodes: H301,H315,H319,H335
• pcodes: P301 + P310 + P330 - P302 + P352 - P305 + P351 + P338
• Hazard Classifications: Acute Tox. 3 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• target_organs: Respiratory system
• Storage Class: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable