Skip to main content
. Author manuscript; available in PMC: 2020 May 1.
Published in final edited form as: Pharmacol Ther. 2020 Jan 28;209:107497. doi: 10.1016/j.pharmthera.2020.107497

Table 2.

Small molecule TRPC3, C6, C7 antagonists.

Namea Structure Target Concentration or IC50 Reference
GSK2332255B
(GSK255B)
graphic file with name nihms-1563237-t0019.jpg TRPC3
TRPC6
IC50, 5 nM
IC50, 4 nM
Seo et al., 2014
GSK2833503A
(GSK503A)
graphic file with name nihms-1563237-t0020.jpg TRPC3
TRPC6
IC50, 21 nM
IC50, 3 nM
Seo et al., 2014
BI 749327 graphic file with name nihms-1563237-t0021.jpg TRPC3
TRPC6
TRPC7
IC50, 1,100 nM
IC50, 13 nM
IC50, 550 nM
Lin et al., 2019
Anilino-thiazoles graphic file with name nihms-1563237-t0022.jpg TRPC3
TRPC6
100 nM
16 nM
Washburn et al., 2013
SAR7334 graphic file with name nihms-1563237-t0023.jpg TRPC3
TRPC6
TRPC7
IC50, 282 nM
IC50, 7.9 nM
IC50, 226 nM
Maier, et al., 2015
BTDM graphic file with name nihms-1563237-t0024.jpg TRPC3
TRPC6
IC50, 11 nM
IC50, 10 nM
Tang, et al., 2018
Larixyl acetate graphic file with name nihms-1563237-t0025.jpg TRPC3
TRPC6
TRPC7
12 fold > C6
IC50, ~0.1 μM
5 fold > C6
Urban et al., 2016
SH045 graphic file with name nihms-1563237-t0026.jpg TRPC3
TRPC6
TRPC7
13 fold > C6
IC50, ~5.8 nM
3.5 fold > C6
Hafner et al., 2018
Pyrazolopyrimidines 14a graphic file with name nihms-1563237-t0027.jpg TRPC6 IC50, 1 μM Ding et al., 2018
Pyr10 graphic file with name nihms-1563237-t0028.jpg TRPC3
TRPC6
IC50, 0.72 μM
IC50 ≥ 10 μM
Schleifer et al., 2012
Pyr3 graphic file with name nihms-1563237-t0029.jpg TRPC3 IC50, 0.7 μM Kiyonaka et al., 2009; Koenig et al., 2013
DS88790512 graphic file with name nihms-1563237-t0030.jpg TRPC6 IC50, 11 nM Motoyama, et al., 2018
Salvianolic acid B graphic file with name nihms-1563237-t0031.jpg TRPC3
TRPC6
27.8 μM Chen et al., 2017b
Sodium tanshinone IIA sulfonate (STS) graphic file with name nihms-1563237-t0032.jpg Attenuated TRPC6, C1 upregulation 12.5 μM Wang et al., 2013a
Jiang et al., 2016a.
Ribemansides A graphic file with name nihms-1563237-t0033.jpg TRPC6 IC50, 24.5 μM Zhou et al., 2018
Ribemansides B graphic file with name nihms-1563237-t0034.jpg TRPC6 IC50, 25.6 μM Zhou et al., 2018
Topotecan (TPT), graphic file with name nihms-1563237-t0035.jpg Suppressed expression of TRPC6 1–10 nM Jiang et al., 2018
FK506 graphic file with name nihms-1563237-t0036.jpg Attenuated TRPC6 upregulation 6.2 μM Ma et al., 2015
Rosiglitazone (RSG) graphic file with name nihms-1563237-t0037.jpg Reduced TRPC6, C1 activation 10 μM Wei et al., 2017
Sildenafil graphic file with name nihms-1563237-t0038.jpg Suppressed TRPC6 expression 300 nM Lu et al., 2010
(‑)‑Oleocanthal (OLCT) graphic file with name nihms-1563237-t0039.jpg Suppressed TRPC6 expression 10–20 μM Diez-Bello, et al., 2019
Pioglitazone graphic file with name nihms-1563237-t0040.jpg Suppressed TRPC6 expression 12 mg/kg body weight (in vivo), 1 μM (in vitro) Sonneveld et al., 2017
a

Compounds with selectivity information and likelihood of direct interaction with the channel are highlighted in bold letters and shaded rows.