| Bioactivity | Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity[1]. | ||||||||||||
| Invitro | Eact elicits both itch-and pain- related behaviours in a TRPV1-dependent manner. Eact activates membrane currents in mTRPV1-expressing HEK293T cells in a concentration-dependent manner with an EC50 of 11.6 ± 2.5 μM. TMEM16A activator Eact activates both native and recombinant TRPV1 channels[1]. | ||||||||||||
| Name | Eact | ||||||||||||
| CAS | 461000-66-8 | ||||||||||||
| Formula | C22H24N2O5S | ||||||||||||
| Molar Mass | 428.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Liu S, et al. Eact, a small molecule activator of TMEM16A, activates TRPV1 and elicits pain- and itch-related behaviours. Br J Pharmacol. 2016 Apr;173(7):1208-18. |