Eact is a selective activator of TMEM16A that directly activates TRPV1 channels in sensory nociceptors, producing itch, acute nociception, and thermosensitivity responses.

Physicochemical Properties

Molecular Formula	C22H24N2O5S
Molecular Weight	428.501364707947
Exact Mass	428.141
CAS #	461000-66-8
PubChem CID	3173542
Appearance	White to off-white solid powder
Density	1.237±0.06 g/cm3(Predicted)
Boiling Point	595.9±60.0 ℃(Predicted)
LogP	4.129
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	9
Heavy Atom Count	30
Complexity	520
Defined Atom Stereocenter Count	0
InChi Key	ZUXNHFFVQWADJL-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H24N2O5S/c1-26-11-10-24(22-23-17(14-30-22)15-8-6-5-7-9-15)21(25)16-12-18(27-2)20(29-4)19(13-16)28-3/h5-9,12-14H,10-11H2,1-4H3
Chemical Name	3,4,5-trimethoxy-N-(2-methoxyethyl)-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Eact Eact depends on TRPV1 to elicit itch and associated pain behaviors. With an EC50 of 11.6±2.5 μM, Eact stimulates membrane currents in HEK293T cells expressing mtrpv1 in a concentration-dependent manner. TRPV1 channels are damaged and rearranged when activated by the TMEM16A activator Eact [1].
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~116.69 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3337 mL	11.6686 mL	23.3372 mL
	5 mM	0.4667 mL	2.3337 mL	4.6674 mL
	10 mM	0.2334 mL	1.1669 mL	2.3337 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.