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| | AZP-531 Basic information |
| Product Name: | AZP-531 | | Synonyms: | AZP-531;Livoletide
(AZP-531;AZP-531?, >96%;Livoletide;Cyclo(L-arginyl-L-valyl-L-glutaminyl-L-seryl-L-prolyl-L-α-glutamyl-L-histidyl-L-glutaminyl) | | CAS: | 1088543-62-7 | | MF: | C40H63N15O13 | | MW: | 962.02 | | EINECS: | | | Product Categories: | | | Mol File: | 1088543-62-7.mol |  |
| | AZP-531 Chemical Properties |
| density | 1.61±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (103.95 mM) | | form | Solid | | pka | 4.46±0.10(Predicted) | | color | White to off-white | | Sequence | Cyclo(Arg-Val-Gln-Ser-Pro-Glu-His-Gln） |
| | AZP-531 Usage And Synthesis |
| Uses | AZP-531 is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. | | 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)[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]. | | References | [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. DOI:10.1016/j.ejps.2012.07.014
[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. DOI:10.1096/fj.12-221143
[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. DOI:10.1111/dom.12675 |
| | AZP-531 Preparation Products And Raw materials |
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