Figure 1. Analysis of hGLP1R expression by IHC. Pancreata from wild-type and hGLP1R mice (HO) were stained using an antibody specific for human GLP1R, and only the pancreas from hGLP1R mice (HO) showed hGLP1R positive signal in pancreatic islet.
Figure 2. Validation of the hypoglycemic efficacy of the test compound in humanized GLP-1R mice. The oral glucose tolerance test (OGTT) was performed (n=5), and the test compound showed a better hypoglycemic efficacy (p<0.001). The above data indicated that the GLP-1R humanized mouse is an effective model for diabetes drug screening.
Figure 3. Efficacy study of PF06882961 in hGLP1R mice. PF06882961 has shown significant effect in hGLP1R mice in OGTT study, but no effect in C57BL/6 mice.
Figure 4. Efficacy study of PF06882961 in HFD/STZ induced type II diabetes model in hGLPIR mice. PF06882961 could significant decreases the body weight(A); PF06882961 could significantly decrease fast blood glucose level and AUC in OGTT study (B).