TRPV4 Antagonist

HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively.

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC₅₀s of 2 nM and 40 nM for rTRPV4 and hTRPV4.

GSK205 is a potent, selective TRPV4 antagonist with an IC₅₀ of 4.19  μM for inhibiting TRPV4-mediated Ca²⁺ influx.

RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC₅₀s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.

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.

RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC₅₀s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

PF-05214030 is a TRPV4 antagonist (IC₅₀: 4 and 27nM for hTRPV4 and rTRPV4 respectively). PF-05214030 reverses the reduction in bladder capacity caused by intravesical infusion of a TRPV4 agonist.

RN-1665 is an orally active TRPV4 antagonist that exhibits excellent selectivity for related TRP receptors such as TRPV1, TRPV3 and TRPM8. RN-1665 is a TRPV4 probe for focus screens, with IC50s of 0.26 μM and 0.39 μM for hTRPV4 and rTRPV4 from human and rat, respectively.

GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC₅₀ of 1 nM for hTRPV4.

TRPV4 antagonist 4 is a potent TRPV4 antagonist with an IC₅₀ value of 22.65 nM. TRPV4 antagonist 4 inhibits TRPV4 current. TRPV4 antagonist 4 shows protective effects on acute lung injury.

RN-9893 Hydrochloride is an orally active antagonist of transient receptor potential vanilloid 4 (TRPV4), with IC₅₀ values of 0.42 and 0.66 μM, for humans and rats, respectively.

TRPV4 antagonist 3 is a TRPV4 antagonist (pIC₅₀ = 8.4).

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively.