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AZP-531 (AZP531) is a novel and potent analogue of unacyclated ghrelin with the potential to be used for the treatment of Prader-Willi syndrome, as it can improve glycaemic control and reduce weight.
| ln Vitro |
AZP-531 exhibits a survival impact on human islets and pancreatic b cells that is similar to that of the parent compound UAG. In vitro, AZP-531 exhibits high stability in human plasma. After one day of incubation at 37°C, no degradation was seen [1].
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| ln Vivo |
The majority of samples had concentrations over the quantitation limit of 1 ng/mL, with the highest quantity of this peptide being 4350 ng/mL [1]. Mice who get AZP-531 infusion do not acquire weight when fed a high-fat diet. Treatment with AZP-531 inhibits the pro-inflammatory effects of a high-fat diet, increases the expression of mitochondrial functional markers in brown adipose tissue, and stops the progression of prediabetes. Moreover, AZP-531 inhibits the rise in acyl ghrelin levels brought on by a high-fat diet [2]. AZP-531 was accepted quite well. Pharmacokinetic characteristics for single- and multiple-doses were similar. AZP-531 maximum concentrations are usually reached an hour after dosage. The area under the curve and maximum measured concentration are dose-related. Two to three hours is the usual terminal half-life. Without raising insulin levels, AZP-531 (≥15 μg/kg) markedly raised glucose concentrations, indicating an insulin-sensitizing action. Compared to a placebo, AZP-531 resulted in a mean body weight reduction of 2.6 kg. All groups' glucose levels improved, even the placebo group's, indicating a potential research impact in patients whose baseline conditions were uncontrolled. AZP-531 60 μg/kg can lower body weight by 2.1 kg (placebo: 1.3 kg) and HbA1c by 0.4% (placebo: 0.2%) [3].
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| References |
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| Additional Infomation |
Livoletide is under investigation in clinical trial NCT03790865 (Effects of Livoletide (AZP-531) on Food-related Behaviors in Patients With Prader-Willi Syndrome).
Drug Indication Treatment of Prader-Willi syndrome |
| Molecular Formula |
C40H63N15O13
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|---|---|
| Molecular Weight |
962.0209
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| Exact Mass |
961.472
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| CAS # |
1088543-62-7
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| PubChem CID |
57341282
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.707
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| LogP |
-9.96
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
68
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| Complexity |
1900
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| Defined Atom Stereocenter Count |
8
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| InChi Key |
JXPWLIYXIWGWSA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C40H63N15O13/c1-19(2)31-38(67)51-23(8-11-29(42)58)34(63)53-26(17-56)39(68)55-14-4-6-27(55)37(66)50-24(9-12-30(59)60)33(62)52-25(15-20-16-45-18-47-20)36(65)49-22(7-10-28(41)57)32(61)48-21(35(64)54-31)5-3-13-46-40(43)44/h16,18-19,21-27,31,56H,3-15,17H2,1-2H3,(H2,41,57)(H2,42,58)(H,45,47)(H,48,61)(H,49,65)(H,50,66)(H,51,67)(H,52,62)(H,53,63)(H,54,64)(H,59,60)(H4,43,44,46)
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| Chemical Name |
3-[6,15-bis(3-amino-3-oxopropyl)-12-[3-(diaminomethylideneamino)propyl]-3-(hydroxymethyl)-18-(1H-imidazol-5-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-9-propan-2-yl-1,4,7,10,13,16,19,22-octazabicyclo[22.3.0]heptacosan-21-yl]propanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~100 mg/mL (~103.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (103.95 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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