Livoletide

Research use only, not for human use.

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist; exhibits the same pharmacological profile as UAG both in vitro and in vivo, independently of AG receptor binding; prevents HFD-induced proinflammatory effects, stimulates expression of mitochondrial function markers in brown adipose tissue, and prevents development of a prediabetic metabolic state; also prevents a HFD-induced increase in acyl ghrelin levels.Diabetes Phase 1 Clinical.

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.

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).

AZP-531 | AZP531

GPCR/G Protein

GHSR

GHSR

Metabolic Disease

Diabetes

1088543-62-7

962.036

C40H63N15O13

>98% (HPLC)

DMSO : 100 mg/mL103.95 mM;

O=C(O)CC[C@H](N1)C(N[C@@H](CC2=CN=CN2)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C(C)C)C(N[C@@H](CCC(N)=O)C(N[C@@H](CO)C(N3CCC[C@@]3([H])C1=O)=O)=O)=O)=O)=O)=O)=O

3-((3S,6S,9S,12S,15S,18S,21S,26aS)-6-((1H-imidazol-4-yl)methyl)-9,18-bis(3-amino-3-oxopropyl)-12-(3-guanidinopropyl)-21-(hydroxymethyl)-15-isopropyl-1,4,7,10,13,16,19,22-octaoxohexacosahydropyrrolo[1,2-a][1,4,7,10,13,16,19,22]octaazacyclotetracosin-3-yl)propanoic acid

(-20℃)

With Ice Pack

≥ 2 years