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  3. AZP-531

AZP-531 

Cat. No.: HY-P0231 Purity: 98.76%
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

Size Price Stock Quantity
1 mg USD 120 In-stock
Estimated Time of Arrival: December 31
5 mg USD 430 In-stock
Estimated Time of Arrival: December 31
10 mg USD 700 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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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.
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: 

H2O : 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.
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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Product Name:
AZP-531
Cat. No.:
HY-P0231
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