Table 2.
Pharmacology of CaCC ANO1/TMEM16A Activators.
| Activator | Structure | EC50 (μmol/L) | Test assay | Selectivity | Effect | Ref. |
|---|---|---|---|---|---|---|
| Eact | ![]() |
3 | hANO1-FRT | TRPV1 (+) TRPV4 (+) [Ca2+]i (+) ANO6 (+) |
Pain, Smooth muscle contraction |
66,109, 110, 111 |
| Fact | ![]() |
6 | hANO1-FRT | NR | NR | 109 |
| INO-4995 | ![]() |
NR | hANO1-HEK293 | NR | NR | 112 |
| Resveratrol | ![]() |
48 | mANO1-HEK293T | NR | Smooth muscle contraction |
113 |
| GRb1 | ![]() |
38.4 | mANO1-HEK293 | NR | Smooth muscle contraction |
114 |
| Cinnamaldehyde | ![]() |
9.7 | ANO1-HEK293 | NR | Smooth muscle contraction |
66 |
| Chitosan oligosaccharides | ![]() |
74.5 μg/mL | mANO1-HEK293 | NR | Smooth muscle contraction |
115 |
| ETX001 | NR | 116 nmol/L | hANO1-FRT sANO1-CHO |
[Ca2+]i (/) | Anti-CF | 116 |
| Melittin | C131H229N39O31 | 0.5–2 | hANO1-HEK293 | ANO6 (+) PLA2 (+) |
Phospholipid scrambling through ANO6 but not ANO1 |
66,117 |
+, activation effect; /, no effect; NR, no report.






