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SML0942

GSK2193874

Name: GSK2193874
Brand: SIGMA

≥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

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About This Item

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

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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
to study its effects on murine compact bone-derived osteoblasts(CB-OB)
to study its effects on lung injury post-lipopolysaccharide (LPS) in mice

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.

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