AZP-531
Based on 2 publication(s) in Google Scholar
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.
- Purity: 99.36%
- CAS No.: 1088543-62-7
- Formula: C40H63N15O13
- Molecular Weight:962.02
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) AZP-531
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Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1088543-62-7
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Appearance Solid
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Molecular Weight 962.02
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Formula C40H63N15O13
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Color White to off-white
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Sequence Shortening
Cyclo(RVQSPEHQ)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Elife
Three-dimensional growth of breast cancer cells potentiates the anti-tumor effects of unacylated ghrelin and AZP-531. [Abstract]2020 Jul 15;9:e56913. PMID: 32667883 -
Solvent & Solubility
H2O : 100 mg/mL (103.95 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (103.95 mM); Clear solution; Need ultrasonic
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.0395 mL | 5.1974 mL | 10.3948 mL | 25.9870 mL |
| 5 mM | 0.2079 mL | 1.0395 mL | 2.0790 mL | 5.1974 mL | |
| 10 mM | 0.1039 mL | 0.5197 mL | 1.0395 mL | 2.5987 mL | |
| 15 mM | 0.0693 mL | 0.3465 mL | 0.6930 mL | 1.7325 mL | |
| 20 mM | 0.0520 mL | 0.2599 mL | 0.5197 mL | 1.2993 mL | |
| 25 mM | 0.0416 mL | 0.2079 mL | 0.4158 mL | 1.0395 mL | |
| 30 mM | 0.0346 mL | 0.1732 mL | 0.3465 mL | 0.8662 mL | |
| 40 mM | 0.0260 mL | 0.1299 mL | 0.2599 mL | 0.6497 mL | |
| 50 mM | 0.0208 mL | 0.1039 mL | 0.2079 mL | 0.5197 mL | |
| 60 mM | 0.0173 mL | 0.0866 mL | 0.1732 mL | 0.4331 mL | |
| 80 mM | 0.0130 mL | 0.0650 mL | 0.1299 mL | 0.3248 mL | |
| 100 mM | 0.0104 mL | 0.0520 mL | 0.1039 mL | 0.2599 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.