2 Results for "

GSK1016790A

" in MedChemExpress (MCE) Product Catalog:
Products (2)

2 Results for "GSK1016790A" in MCE Product Catalog:

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39
39 Cited Publications
Cat. No.: HY-19608
CAS No.: 942206-85-1
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEK cells .
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Cat. No.: HY-187364
CAS No.: 3050594-88-9
Research Areas:  

Inflammation/Immunology

TRPV4 antagonist-7 is a potent and selective TRPV4 antagonist with an IC50 of 0.2 nM against human targets. TRPV4 antagonist-7 binds to the voltage-sensor-like domain cavity of TRPV4 and inhibits channel activity through the formation of salt bridges, hydrogen bonds, and edge-to-face π-stacking interactions. TRPV4 antagonist-7 induces phospholipid accumulation in HepG2 C3A cells in vitro with an IC50 of 3.8 μM, and exhibits moderate inhibitory effects on CYP2D6 with an IC50 of 5.1 μM. TRPV4 antagonist-7 dose-dependently inhibits GSK1016790A (HY-19608)-induced bronchoconstriction in rats and cough in guinea pigs. TRPV4 antagonist-7 can be used in studies related to respiratory system diseases .
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