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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

Quality level:

100

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Product Name

GSK2193874, ≥98% (HPLC)

Quality Level

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

Related Categories

Bioactive Small Molecule Inhibitors

Bioactive Small Molecules

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

Not applicable

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PAR2-Mediated cAMP Generation Suppresses TRPV4-Dependent Ca2+ Signaling in Alveolar Macrophages to Resolve TLR4-Induced Inflammation.

Sheikh Rayees et al.

Cell reports, 27(3), 793-805 (2019-04-18)

Alveolar macrophages (AMs), upon sensing pathogens, trigger host defense by activating toll-like receptor 4 (TLR4), but the counterbalancing mechanisms that deactivate AM inflammatory signaling and prevent lethal edema, the hallmark of acute lung injury (ALI), remain unknown. Here, we demonstrate

TRPV4 Channel Signaling in Macrophages Promotes Gastrointestinal Motility via Direct Effects on Smooth Muscle Cells.

Jialie Luo et al.

Immunity, 49(1), 107-119 (2018-07-01)

Intestinal macrophages are critical for gastrointestinal (GI) homeostasis, but our understanding of their role in regulating intestinal motility is incomplete. Here, we report that CX3C chemokine receptor 1-expressing muscularis macrophages (MMs) were required to maintain normal GI motility. MMs expressed the

A Novel Pro-Inflammatory Mechanosensing Pathway Orchestrated by the Disintegrin Metalloproteinase ADAM15 in Synovial Fibroblasts.

Tomasz Janczi et al.

Cells, 10(10) (2021-10-24)

Mechanotransduction is elicited in cells upon the perception of physical forces transmitted via the extracellular matrix in their surroundings and results in signaling events that impact cellular functions. This physiological process is a prerequisite for maintaining the integrity of diarthrodial

TRPV4 Inhibition and CRISPR-Cas9 Knockout Reduce Inflammation Induced by Hyperphysiological Stretching in Human Annulus Fibrosus Cells.

Elena Cambria et al.

Cells, 9(7) (2020-07-28)

Mechanical loading and inflammation interact to cause degenerative disc disease and low back pain (LBP). However, the underlying mechanosensing and mechanotransductive pathways are poorly understood. This results in untargeted pharmacological treatments that do not take the mechanical aspect of LBP

Mechanically stimulated ATP release from murine bone cells is regulated by a balance of injury and repair.

Nicholas Mikolajewicz et al.

eLife, 7 (2018-10-17)

Bone cells sense and actively adapt to physical perturbations to prevent critical damage. ATP release is among the earliest cellular responses to mechanical stimulation. Mechanical stimulation of a single murine osteoblast led to the release of 70 ± 24 amole

Global Trade Item Number

SKU	GTIN
SML0942-25MG	04061832560427
SML0942-5MG	04061832560434

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