Bioactivity | T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC)[1][2]. | |||||||||
Target | TMEM16A. | |||||||||
Invitro | T16Ainh-A01 (0.3-30 μM) significantly reduces both inward and outward components of IClCa, and inhibits IClCa in RUICC without significantly affecting L-type Ca2+ current[1].T16Ainh-A01 (10 μM) inhibits nearly completely TMEM16A chloride current (induced by 275 nM free calcium in the pipette) at all voltages, indicating a voltage-independent block mechanism[2]. | |||||||||
Name | T16Ainh-A01 | |||||||||
CAS | 552309-42-9 | |||||||||
Formula | C19H20N4O3S2 | |||||||||
Molar Mass | 416.52 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Fedigan S, et al. Effects of new-generation TMEM16A inhibitors on calcium-activated chloride currents in rabbit urethral interstitial cells of Cajal. Pflugers Arch. 2017 Nov;469(11):1443-1455. [2]. Namkung W, et al. TMEM16A inhibitors reveal TMEM16A as a minor component of calcium-activated chloride channel conductance in airway and intestinal epithelial cells. J Biol Chem. 2011 Jan 21;286(3):2365-74. |