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|---|---|---|
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| Cat. No. : | HY-B1177 |
| M.Wt: | 203.28 |
| Formula: | C13H17NO |
| Purity: | >98 % |
| Solubility: | DMSO : 140 mg/mL (ultrasonic);H2O : 140 mg/mL (ultrasonic) |
Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus[1][2].
In Vitro:Crotamiton (0-500 μM) potently inhibits GSK1016790A-activated mTRPV4 currents in HEK293T cells under the condition of 2 mM extracellular Ca2+ in vitro, with IC50 values of 15.5 μM and 16.3 μM in mouse and human, respectively[1].
Crotamiton (100-1000 μM) inhibits mTRPV4 currents activated by GSK1016790A in HEK293T cells cultured in calcium-free medium, with an IC50 of 223.5 μM[1].
Crotamiton (0-1000 μM) inhibits TRPV4 currents in GSK1016790A-activated NHEK cells in calcium-free medium[1].
Crotamiton (0-1000 μM) reduces the open probability and unitary amplitude of mTRPV4 single channels in HEK293T cells[1].
Washout after co-treatment with Crotamiton (0-1000 μM; 60 s, co-applied with GSK1016790A) and GSK1016790A induces dilation of the mTRPV4 channel in HEK293T cells, which allows the permeation of large cations up to TetMA+ (6.48 Å diameter), but does not permit the permeation of NMDG (8.90 Å diameter)[1].
Crotamiton (1 mM; 5 min pre-incubation) inhibits histamine (HY-B1204)- and chloroquine (HY-17589A)-induced calcium influx in HEK293T cells expressing H1R/TRPV1 or MRGPRA3/TRPA1, with IC50 values of 101.2 μM and 326.2 μM, respectively. Its mechanism of action functions through the H1R/TRPV1 pathway, rather than directly inhibiting TRPV1[2].
In Vivo:Topical administration of a single dose of Crotamiton (30 μL) significantly inhibits TRPV4 agonist (GSK1016790A) (HY-19608)-induced pruritus-related scratching behavior in C57BL/6N mice[1].
Crotamiton (i.p., 125 mg/kg, single dose) reduces histamine- and chloroquine-induced scratching episodes in male ICR mice[2].
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