Table 2 NEP 24.11 and mouse plasma degradation assays

From: Peptide-oligourea hybrids analogue of GLP-1 with improved action in vivo

 

Compound

Potency (%)a

NEP 24.11 t1/2 (h)b

SEM (h)c

Mouse plasma t1/2 (min)d

SEM (min)e

In vivo activityf

1

GLP-1-G2-NH2 (GG2)

100

3.6

0.1

16

1

+

2

GG2[DuαAuAu]9,10,11,12

2

4.4

0.4

17

1

 

5

GG2[AuYuAu]11,12,13,14

15

2.9

0.3

23

3

+

9

GG2[YuEuAu]14,15,16,17

135

3.0

0.2

17

1

+

11

GG2[EuAuAu]15,16,17,18

13

3.9

0.4

31*

3

 

14

GG2[AuAuAu]18,19,20,21

6

4.9

0.8

38***

2

+++

16

GG2[FuαIuAu]22,23,24,25

0.4

1.8

0.1

38***

5

 

22

GG2[AuAuAu]28,29,30,31

19

4.5

0.5

>60***

na

+++

23

GG2[YuEuAuAuAuAu]14,15,16,17,18,19,20,21

7

6.1*

0.9

39***

5

+++

  1. Statistic by one-way ANOVA with Dunnett’s multiple comparison test: *p  < 0.05; ***p < 0.001, comparing peptide 1 to oligomers. Source data are provided as a Source Data file
  2. aPercentage of potency (cAMP production) compared to GLP-1-G2 (see Fig. 2)
  3. bHalf-life of GLP-1 analogue in NEP 24.11 degradation assay: mean value of three replicates (n  = 3)
  4. cStandard error of the mean on the NEP 24.11 t1/2
  5. dHalf-life of GLP-1 analogue in mouse plasma degradation assay: mean value of four replicates (n  = 4)
  6. eStandard error of the mean on the mouse plasma t1/2
  7. fIndicator of in vivo activity: + active, + + + more active
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