Fig. 1 · Structure

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GSK-2193874

Cat. No. A14201 CAS 1336960-13-4

TRPV4 blocker

GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
HEK293 IC50 0.04 μM Antagonist activity at human TRPV4 expressed in HEK293 cells assessed as inhibition of GSK634775A-induced calcium influx preincubated for 10 mins followed by GSK634775A addition by Fura-4 dye based FLIPR assay [PMID: 28523109]

Specifications

Manufacturer Adooq Bioscience
Actions Blocker
CAS Number 1336960-13-4
Applications TRPV4 blocker
Formula C37H38BrF3N4O
Molecular Weight 691.62
SMILES
C1CCN(CC1)C2CCN(CC2)CC3=C(N=C4C=C(C=CC4=C3C(=O)NC5(CC5)C6=CC=CC=C6)Br)C7=CC(=CC=C7)C(F)(F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 95 mg/mL (137.35 mM)
Water Insoluble
Ethanol Warmed: 48 mg/mL (69.4 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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