Petrelintide acetate
Based on 1 Customer Validation
Perelintide (ZP8396) acetate is a dual amylin and calcitonin receptor agonist (DACRA). Perelintide acetate elicits a selective reduction in high-fat diet intake in diet-induced obese (DIO) rats, which is accompanied by a loss of fat mass and preservation of lean mass during weight reduction. Perelintide acetate can be utilized in diabetes research.
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- Pureza : 99.88%
- Fòrmula: C185H305N49O61.xC2H4O2
- Peso molecular:4191.69 (free base)
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Almacenamiento:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
hAMY3R 2.997 nM (EC50) |
hCTR 9.215 nM (EC50) |
In Vitro
Petrelintide acetate demonstrates agonistic activity against hAMY3R and hCTR in HEK-293 cells, with EC50 of 2.997 and 9.215 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ |
|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | s.c. | 26.2 h | 24 h | 4850 ng/mL | 254046 ng·h/mL | 286517 ng·h/mL |
In Vivo
Petrelintide (2 nmol/kg, s.c., every second day for 30 days, or 10 nmol/kg, s.c., every fourth day for 30 days) acetate reduces food intake and body weight in DIO rats primarily by lowering intake of high fat diet[2].
Petrelintide (2 nmol/kg, s.c., every second day for 30 days, or 10 nmol/kg, s.c., every fourth day for 30 days) acetate shows preferential fat mass loss and preservation of relative lean mass during weight loss in DIO rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DIO rats[1]
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Dosage:0.04 mg/kg
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Administration:s.c., every third day for a total of 10 doses
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Result:Significantly reduced body weight and food intake compared to the vehicle group.
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Animal Model:DIO rats[2]
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Dosage:2, 10 nmol/kg
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Administration:s.c., every second day (2 nmol/kg) or every fourth day (10 nmol/kg) for 30 days
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Result:Resulted in significant lower relative body weight compared to vehicle.
Resulted in significant reduction of total cumulative intake of high fat diet compared to vehicle.
Exhibited no change in total cumulative intake of chow compared to vehicle.
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Animal Model:DIO rats[3]
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Dosage:2, 10 nmol/kg
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Administration:s.c., every second day (2 nmol/kg) or every fourth day (10 nmol/kg) for 30 days
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Result:Resulted in significantly lower relative body weight compared to vehicle.
Resulted in significant reduction of fat mass in comparison to vehicle.
Resulted in significant preservation of relative lean mass in comparison to vehicle.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Peso molecular 4191.69 (free base)
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Fòrmula C185H305N49O61.xC2H4O2
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Color White to off-white
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Synonyms
ZP8396 acetate
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Sequence
{γGlu-arachidate}-Arg-Asp-Gly-Thr-Ala-Thr-Lys-Ala-Thr-Glu-Arg-Leu-Ala-{homoGlu}-Phe-Leu-Gln-Arg-Ser-Ser-Phe-{Sar}-Ala{NMeIle}-Leu-Ser-Ser-Thr-Glu-Val-Gly-Ser-Asn-Thr-{Hyp}-NH2 (Lactm bridge:Asp3-Lys8)
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Sequence Shortening
{γGlu-arachidate}-RDGTATKATERLA-{homoGlu}-FLQRSSF-{Sar}-A{NMeIle}-LSSTEVGSNT-{Hyp}-NH2 (Lactm bridge:Asp3-Lys8)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- 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: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Pureza y Documentación
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Ficha de datos (296 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Petrelintide acetate Related Classifications
HY-P10745A Related Classifications
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