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AZP-531
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:1088543-62-7
规格:98%
分子量:962.02
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
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。
CAS:1088543-62-7
分子式:C40H63N15O13
分子量:962.02
纯度:98%
存储:Store at -20°C

Background:

AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight.


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[1].


The highest concentration of this peptide is 4350 ng/mL, and the majority of samples are above the limit of quantification (1 ng/mL)[1]. 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[2]. 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)[3].


[1]. Julien M, et al. In vitro and in vivo stability and pharmacokinetic profile of unacylated ghrelin (UAG) analogues. Eur J Pharm Sci. 2012 Nov 20;47(4):625-35. [2]. Delhanty PJ, et al. Des-acyl ghrelin analogs prevent high-fat-diet-induced dysregulation of glucosehomeostasis. FASEB J. 2013 Apr;27(4):1690-700. [3]. Allas S, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of AZP-531, a first-in-class analogue of unacylated ghrelin, in healthy and overweight/obese subjects and subjects with type 2 diabetes. Diabetes Obes Metab. 2016 Sep;18(9):868-74.