Table 1 NN9056 binding and activation of porcine and human CCK-1 and CCK-2 receptors

From: Long-acting CCK analogue NN9056 lowers food intake and body weight in obese Göttingen Minipigs

 

CCK-1 receptor

CCK-2 receptor

 

NN9056

CCK-8

NN9056

CCK-8

Binding

Mean IC50 (nM)

95% CI (nM)

Mean IC50 (nM)

95% CI (nM)

Mean IC50 (nM)

95% CI (nM)

Mean IC50 (nM)

95% CI (nM)

Pig

0.123

0.037–0.406

0.199

0.173–0.211

>125a

N/A

0.102

0.039–0.262

Human

0.105

0.099–0.111

0.203

0.137–0.302

>125a

N/A

1.876

0.823–4.277

Activation

Mean EC50 (nM)

95% CI (nM)

Mean EC50 (nM)

95% CI (nM)

Mean EC50 (nM)

95% CI (nM)

Mean EC50 (nM)

95% CI (nM)

Pig

0.205

0.073–0.573

0.221

0.146–0.335

>100b

N/A

0.325

0.241–0.438

Human

0.093

0.059–0.147

0.059

0.041–0.085

>100b

N/A

0.367

0.300–0.448

  1. Data are presented as mean with 95% CIs, n = 3
  2. CI confidence interval, IC50 half-maximal inhibitory concentration, EC50 half-maximal effective concentration
  3. aMean IC50 is designated as >125 nM because the IC50 values from the individual experiments were larger than the highest compound dose tested (125 nM) or could not be determined by GraphPad Prism
  4. bMean EC50 is designated as >100 nM because the EC50 values from the individual experiments were larger than the highest compound dose tested (100 nM) or could not be determined by GraphPad Prism