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AZP-531

CAS No. : 1088543-62⁻⁷

MCE 国际站：AZP-531

产品活性：AZP-531是一种用于提高血糖控制并减轻体重的非格酸化生长素释放肽类似物。

研究领域：GPCR/G Protein

作用靶点：GHSR

In Vitro: AZP-531 exerts survival effects on pancreatic b-cells and human pancreatic islets which is comparable to that of UAG, the parent molecule. AZP-531 is very stable in human plasma in vitro. No degradation is observed after 1 day of incubation at 37°C.

In Vivo: The highest concentration of this peptide is 4350 ng/mL, and the majority of samples are above the limit of quantification (1 ng/mL). AZP-531 infusion prevents the increase in body weight caused by high-fat diet in mice. AZP-531 treatment prevents high-fat diet-induced proinflammatory effects, stimulates expression of mitochondrial function markers in brown adipose tissue, and prevents development of a prediabetic metabolic state. AZP-531 also prevents a high-fat diet-induced increase in acyl ghrelin levels. AZP-531 is well tolerated. Single- and multiple-dose pharmokinetic variables are similar. Maximum AZP-531 concentrations are typically reached at 1 h post-dose. Observed maximum concentration and area under the curve are dose-proportional. The mean terminal half-life is 2–3 h. AZP-531 (≥15 µg/kg) significantly improves glucose concentrations, without increasing insulin levels, suggesting an insulin-sensitizing effect. AZP-531 decreases mean body weight by 2.6 kg (vs 0.8 kg for placebo). Glucose variables improve in all groups, including placebo, suggesting a study effect in uncontrolled patients at baseline. AZP-531 60 µg/kg reduces HbA1c by 0.4% (vs 0.2% for placebo) and body weight by 2.1 kg (vs 1.3 kg for placebo).

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