TABLE 1

In vitro potency values for sweet-tasting compounds

Potencies (EC50 values) of tastant agonists of human TAS1R2/R3 obtained from concentration-response functions in fluorescence calcium imaging cell-based assay. In many cases, potency values were not explicitly stated in the literature cited. When not explicitly stated, EC50 values have been approximated by visual inspection of concentration-response curves shown in the figures from those papers (italicized in the table).

TastantEC50Reference
Sucrose∼60 mM (Graph, Fig. 2C), without Gα15Li et al. (2002)
∼30 mM (Graph, Fig. 2D), with Gα15
∼60 mM (Graph, Fig. 4b)Zhang et al. (2010)
62 mMServant et al. (2010)
54 mM
∼30 mM (Graph, Fig. 2B)Xu et al. (2004)
19.4 mM (in Supporting Information, caption to Fig. 6)
Sucralose27 μMShimizu et al. (2014)
∼100 µM (Graph, Fig. 2a)Zhang et al. (2010)
∼100 µM (Graph, Fig. 2c)
∼200 µM (Graph, Supporting Information, Fig. S2A)
60 µMServant et al. (2010)
120 µM
59 µM
74 µM
39 µM
36 µM
31 µM
36 µM
62 µM
62 µM
Saccharin∼200 µM (Graph, Fig. 2C), without Gα15Li et al. (2002)
∼60 µM (Graph, Fig. 2D), with Gα15
300 µMSanematsu et al. (2014)
370 µMImada et al. (2010)
42 µM (in Supporting Information, caption to Fig. 6)Xu et al. (2004)
ACE K120 µMWinnig et al. (2007)
940 µMImada et al. (2010)
Aspartame∼2 mM (Graph, Fig. 2C), without Gα15Li et al. (2002)
∼0.5 mM (Graph, Fig. 2D), with Gα15
500 µMWinnig et al. (2007)
1.3 mM
1.2 mMImada et al. (2010)
5 mMLiu et al. (2011)
∼0.3 mM (Graph, Fig. 2B)Xu et al. (2004)
245 µM (in Supplemental Table 1)Maillet et al. (2015)
d-Tryptophan3.3 mMJiang et al. (2005b)
4.3 mMJiang et al. (2005a)
∼3 mM (Graph, Fig. 2C), without Gα15Li et al. (2002)
∼0.8 mM (Graph, Fig. 2D), with Gα15
∼7 mM (Graph, Fig. 4b)Zhang et al. (2010)
370 μM (in Supporting Information, caption to Fig. 6)Xu et al. (2004)
Cyclamate∼2 mM (Graph, Figs. 4C and 5E)Shimizu et al. (2014)
3.1 mMJiang et al. (2005b)
1.86 mM (in Supplemental Table 1)Maillet et al. (2015)
∼3 mM (Graph, Fig. 4b)Zhang et al. (2010)
2.2 mMWinnig et al. (2007)
4.6 mMImada et al. (2010)
∼0.5 mM (Graph, Fig. 2B)Xu et al. (2004)
Monellin11.3 µMJiang et al. (2004)
Brazein86.6 µMJiang et al. (2004)
Neotame∼500 nM (Graph, S1A)Servant et al. (2010)
14 μMLiu et al. (2011)
∼2 μM (Graph, Fig. 2B)Xu et al. (2004)