1. GPCR/G Protein
  2. GHSR
  3. AZP-531

AZP-531 

Cat. No.: HY-P0231
Handling Instructions

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

For research use only. We do not sell to patients.

Custom Peptide Synthesis

AZP-531 Chemical Structure

AZP-531 Chemical Structure

CAS No. : 1088543-62-7

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1 mg USD 144 Ask For Quote & Lead Time
5 mg USD 576 Ask For Quote & Lead Time
10 mg USD 936 Ask For Quote & Lead Time

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Description

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

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

962.02

Formula

C₄₀H₆₃N₁₅O₁₃

CAS No.

1088543-62-7

Sequence

Cyclo(Arg-Val-Gln-Ser-Pro-Glu-His-Gln)

Sequence Shortening

Cyclo(RVQSPEHQ)

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (103.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0395 mL 5.1974 mL 10.3948 mL
5 mM 0.2079 mL 1.0395 mL 2.0790 mL
10 mM 0.1039 mL 0.5197 mL 1.0395 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1][2]

Rats: AZP-531 is administered in sterile water to obtain a 1 mg/kg and 0.3 mg/kg dose in the rat through both intravenous and subcutaneous routes. Blood is collected at t=0, 2, 5, 15, 30, 60, 120, 240, 360, 480 and 1440 min post-administration for the intravenous dose route and t=0, 15, 30, 60, 120, 240, 360, 480 and 1440 min post-administration for the subcutaneous route[1].

Mice: AZP531 is prepared in saline. C57BL/6J mice are infused with saline, DAG, or AZP531 continuously for 4 weeks, and fed either normal diet (ND) or normal diet for 2 weeks followed by a high-fat diet (HFD) for 2 weeks. Peptides are infused at 4 nM/kg/h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

AZP-531AZP531AZP 531GHSRGrowth hormone secretagogue receptorInhibitorinhibitorinhibit

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