GSK 2193874 - 98%, high purity , CAS No.1336960-13-4, Channel blocker of TRPV4

Item Number
G287297
Grouped product items
SKUSizeAvailabilityPrice Qty
G287297-5mg
5mg
In stock
$90.90
G287297-10mg
10mg
In stock
$155.90
G287297-25mg
25mg
In stock
$312.90
G287297-50mg
50mg
In stock
$508.90
G287297-100mg
100mg
In stock
$900.90

Potent and selective TRPV4 antagonist; orally active

View related series
TRPV4 Channel blocker

Basic Description

SynonymsGSK2193874 | GSK-2193874 | GTPL6465 | NCGC00370767-01 | CS-7612 | 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-(3-(trifluoromethyl)phenyl)quinoline-4-carboxamide | BS-15222 | AC-33151 | SCHEMBL2404540 | BDBM50232797 | 7-bromo-N-(1-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent and selective TRPV4 antagonist (IC50values are 2 and 40 nM for rat and human receptors, respectively); inhibits Ca2+influx through TRPV4 channels. Prevents and reverses pulmonary edema after myocardial infarctionin vivomodels. Selective over a pane
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeCHANNEL BLOCKER
Mechanism of actionChannel blocker of TRPV4

Associated Targets(Human)

TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (7 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TRPV1 Tclin Vanilloid receptor (8273 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRPV4 Tchem Transient receptor potential cation channel subfamily V member 4 (774 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRPC3 Tchem Short transient receptor potential channel 3 (70 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Canis familiaris (36305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpa1 Transient receptor potential cation channel subfamily A member 1 (1003 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpm8 Transient receptor potential cation channel subfamily M member 8 (889 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpc6 Short transient receptor potential channel 6 (57 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CACNA1C Voltage-dependent L-type calcium channel subunit alpha-1C (242 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 7-bromo-N-(1-phenylcyclopropyl)-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide
INCHI 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
Canonical SMILES C1CCN(CC1)C2CCN(CC2)CC3=C(C4=C(C=C(C=C4)Br)N=C3C5=CC(=CC=C5)C(F)(F)F)C(=O)NC6(CC6)C7=CC=CC=C7
Isomeric SMILES C1CCN(CC1)C2CCN(CC2)CC3=C(C4=C(C=C(C=C4)Br)N=C3C5=CC(=CC=C5)C(F)(F)F)C(=O)NC6(CC6)C7=CC=CC=C7
Alternate CAS 1336960-13-4
PubChem CID 53464483
MeSH Entry Terms 7-bromo-N-(1-phenylcyclopropyl)-3-((4-piperidin-1-ylpiperidin-1-yl)methyl)-2-(3-(trifluoromethyl)phenyl)quinoline-4-carboxamide;GSK2193874
Molecular Weight 691.62

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
K2215402Certificate of AnalysisAug 11, 2022 G287297
K2215404Certificate of AnalysisAug 11, 2022 G287297
K2215405Certificate of AnalysisAug 11, 2022 G287297
K2215406Certificate of AnalysisAug 11, 2022 G287297
K2215407Certificate of AnalysisAug 11, 2022 G287297

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 34.58, Max Conc. mM: 50

Safety and Hazards(GHS)

Pictogram(s) GHS06
Signal Danger
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P301+P310:IF SWALLOWED: Immediately call a POISON CENTER/doctor/...

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