Capromorelin Tartrate
Based on 1 Customer Validation
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki of 7 nM for hGHS-R1a.
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- Pureza: 98.10%
- No. CAS: 193273-69-7
- Fòrmula: C32H41N5O10
- Peso molecular:655.70
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Actividad biológica
Ki: 7 nM (hGHS-R1a)[2]
Capromorelin stimulates GH release in rat pituitary cell cultures with EC50 of 3 nM[2].
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.
Chemical Information
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No. CAS 193273-69-7
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Appearance Solid
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Peso molecular 655.70
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Fòrmula C32H41N5O10
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Color White to off-white
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SMILES
O=C([C@@H]([C@@H](O)C(O)=O)O)O.CC(C)(N)C(N[C@H](COCC1=CC=CC=C1)C(N(C[C@]23CC4=CC=CC=C4)CCC2=NN(C)C3=O)=O)=O
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Synonyms
CP 424391-18
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
H2O : 100 mg/mL (152.51 mM; Need ultrasonic)
DMSO : 100 mg/mL (152.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.81 mM); 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.81 mM); 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.
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: 50 mg/mL (76.25 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocolo
Membranes are prepared from HEK293 cells (ATCC) stably transfected with the human GHS-R1a receptor cDNA in the plasmid pcDNA3.1neo. Competition radioligand binding assays are performed in 96-well format with GF/C filters pre-soaked in 0.3% polyethyleneimine. Assays are performed at room temperature for 1 h in duplicate using 50 pM [125I]-ghrelin and 1 μg membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2, 0.2% bovine serum albumin and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The membranes are harvested and washed three times with ice-cold ish buffer containing 50 mM HEPES, pH 7.4 and 10 mM MgCl2. IC50 and Ki values are determined using Prism by GraphpadTM. The Kd of [125I]-ghrelin at membranes expressing human GHS receptors is calculated to be 0.2 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The study tested capromorelin flavored oral solution with 30 mg/mL of capromorelin compared to a matched placebo flavored oral solution treatment (which contains all the ingredients of the formulation without capromorelin) administered for 4 days. Dogs are randomized into two groups, with Group 1 receiving placebo (0.1 mL/kg) and Group 2 receiving 3.0 mg/kg. Both groups are treated once a day at approximately 9 AM each day. The first day of dosing is considered Day 0. The placebo and test drug are administered by a syringe placed in the corner of the mouth. The Day 0 weight is used for dose calculations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Zollers B, et al. Capromorelin oral solution (ENTYCE?) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study. BMC Vet Res. 2017 Jan 5;13(1):10. [Content Brief]
[2]. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. [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 / DMSO | 1 mM | 1.5251 mL | 7.6254 mL | 15.2509 mL | 38.1272 mL |
| 5 mM | 0.3050 mL | 1.5251 mL | 3.0502 mL | 7.6254 mL | |
| 10 mM | 0.1525 mL | 0.7625 mL | 1.5251 mL | 3.8127 mL | |
| 15 mM | 0.1017 mL | 0.5084 mL | 1.0167 mL | 2.5418 mL | |
| 20 mM | 0.0763 mL | 0.3813 mL | 0.7625 mL | 1.9064 mL | |
| 25 mM | 0.0610 mL | 0.3050 mL | 0.6100 mL | 1.5251 mL | |
| 30 mM | 0.0508 mL | 0.2542 mL | 0.5084 mL | 1.2709 mL | |
| 40 mM | 0.0381 mL | 0.1906 mL | 0.3813 mL | 0.9532 mL | |
| 50 mM | 0.0305 mL | 0.1525 mL | 0.3050 mL | 0.7625 mL | |
| 60 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6355 mL | |
| 80 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.4766 mL | |
| 100 mM | 0.0153 mL | 0.0763 mL | 0.1525 mL | 0.3813 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.
Capromorelin Tartrate Related Classifications
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