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Table 1 EC50 values of PAR agonists in A431. EC50 values were obtained using conventional Ca2+ flux assay, in comparison with those obtained using the MRCAT. In the case of MRCAT data, the amplitudes of both P-DMR and N-DMR events as a function of agonist concentration (as indicated in Fig. 1c) were used to calculate EC50.

From: Optical biosensor differentiates signaling of endogenous PAR1 and PAR2 in A431 cells

Ligand

EC50(n = 3)

 

Ca2+flux assay

P-DMR

N-DMR

Trypsin

45.7 ± 5.8 nM

98.0 ± 27.8 nM

102.1 ± 21.9 nM

SLIGRL-amide

2.5 ± 0.3 μM

2.3 ± 0.6 μM

3.2 ± 0.8 μM

SLIGKV-amide

3.8 ± 0.4 μM

6.1 ± 1.0 μM

9.1 ± 2.2 μM

Thrombin

6.0 ± 1.0 unit/ml

9.6 ± 2.0 unit/ml

11.0 ± 1.9 unit/ml

SFLLR-amide

5.0 ± 0.4 μM

1.9 ± 0.1 μM

3.1 ± 0.2 μM