GSK1016790A
CAS No. : 942206-85-1
| Size | Price | Stock |
|---|---|---|
| 5mg | $83 | In-stock |
| 10mg | $143 | In-stock |
| 25mg | $308 | In-stock |
| 50mg | $545 | In-stock |
| 100mg | $902 | In-stock |
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| Cat. No. : | HY-19608 |
| M.Wt: | 655.61 |
| Formula: | C28H32Cl2N4O6S2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 33 mg/mL;Methanol : 50 mg/mL (ultrasonic) |
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca2+ influx and elevate intracellular Ca2+ in HEK cells[1][2].
In Vitro: GSK1016790A (0.1-1000 nM) elicits Ca2+ influx in mouse and human TRPV4-expressing human embryonic kidney (HEK) cells (EC50 values of 18 and 2.1 nM, respectively) and it evokes a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. GSK1016790A (100 nM) treatment elicits a rapid elevation of intracellular Ca2+ in a subset of neurons[2].
In Vivo: GSK1016790A (0.001-0.1 mg/kg; i.p.) produces a dose-dependent inhibitory effect on whole gut transit time in mice[2].
GSK1016790A (0.1-1000 nM; pretreatment 10 min) significantly inhibits the electrical field stimulation (EFS)-induced twitch contractions in isolated mouse colon strips in a concentration-dependent manner[2].
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