PK profile of orally dosed peptides in monkeys.

<p>[Leu¹⁴]exenatide-ABD (▾) and [Leu¹⁴]exenatide-ABP (▿), n = 3. Data are presented as mean ± SEM.</p

Functional activity at the GLP-1 receptor.

<p>GLP-1 (7–36) (▪), [Leu¹⁴]exenatide-ABD (▾) and [Leu¹⁴]exenatide-ABP (▿). GLP-1 (7–36) was used as a reference standard in the assay. The assay was run in quadruplicates and data are presented as mean ± SD. Abbreviations: Fluorescence (F).</p

Binding Constants for Albumin Interactions at 25°C.

<p>The number in parentheses represents the standard deviation in the last significant digit.</p

Four-week chronic dosing of peptides in diabetic <i>Lep^ob/ob</i> Mice.

<p>(A) effects on HbA1c (B) effects on body weight and (C) effects on food intake. Vehicle (□), [Leu¹⁴]exenatide-ABD (▾) and exenatide (▪). Data are presented as mean ± SEM, n = 10. *p<0.05 vs. vehicle, #p<0.05 vs. exenatide infusion by ANOVA with Tukey’s test.</p

Names and Sequences of Compounds.

<p>Names and Sequences of Compounds.</p

<i>In Vitro</i> Activity, Metabolic Stability, and Plasma Glucose in OGTT.

<p>Stability results (measured as plasma AUC 0–5 h; pancreatin mix AUC 0–2 h)) are expressed as a percentage of peptide remaining versus stable control peptide ± SEM. Replicates within each assay n = 3, except for exenatide and [Leu¹⁴]exenatide-ABP where n = 2.</p

PK profile of intravenously dosed peptides in rats and monkeys.

<p>(A) rats, n = 3–4 and (B) monkeys, n = 3. Exenatide (▪), [Leu¹⁴]exenatide-ABD (▾) and [Leu¹⁴]exenatide-ABP (▿). Data are presented as mean ± SEM.</p