CGP71683 hydrochloride
Based on 1 Customer Validation
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes.
For research use only. We do not sell to patients.
- Purity: 99.44%
- CAS No.: 192322-50-2
- Formula: C26H30ClN5O2S
- Molecular Weight:512.07
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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All Neuropeptide Y Receptor Isoforms
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Biological Activity
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NPY Y5 receptor |
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes[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.
Chemical Information
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CAS No. 192322-50-2
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Appearance Solid
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Molecular Weight 512.07
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Formula C26H30ClN5O2S
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Color White to off-white
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SMILES
O=S(C1=C2C=CC=CC2=CC=C1)(NC[C@H]3CC[C@H](CNC4=NC(N)=C5C=CC=CC5=N4)CC3)=O.Cl
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Synonyms
CGP71683A
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 160 mg/mL (312.46 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.
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.
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: ≥ 2.67 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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.
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.
Protocol
Rats[2]
CGP71683 is dissolved in 30% DMSO and kept frozen at -20°C until the experiment. Each microinjection consists of 2 μL of either vehicle (30% DMSO) or CGP71683 (7.5 nmol/μL; 15 nmol/rat) injected during 30-60 s through the guide cannula, as the following protocols: I - rats with free access to chow receive 6 microinjections (15 nmol/rat, 10-14 h interval between each one) and are killed 1 h after the last injection, between 9 and 10 a.m. Food intake is estimated by the reduction in chow mass (g), evaluated daily, immediately before each icv injection. II - 72 h-fasted rats receive a single microinjection of vehicle or CGP71683 (15 nmol/rat) and sacrificed 1 h latter. III - during a period of 72 h of fasting, rats are treated with multiple injections of vehicle or CGP71683 with the same protocol used for fed animals, and the fasting period started 10 h before the first microinjection. At the end of experimental protocols, rats are decapitated and serum is obtained from trunk blood for the measurement of the concentrations of hormones[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 (274 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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Handling Instructions (2659 KB)
References
[1]. Lecklin A, et al. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37. [Content Brief]
[2]. Costa-e-Sousa RH, et al. Central NPY-Y5 receptors activation plays a major role in fasting-induced pituitary-thyroid axis suppression in adult rat. Regul Pept. 2011 Nov 10;171(1-3):43-7. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9529 mL | 9.7643 mL | 19.5286 mL | 48.8214 mL |
| 5 mM | 0.3906 mL | 1.9529 mL | 3.9057 mL | 9.7643 mL | |
| 10 mM | 0.1953 mL | 0.9764 mL | 1.9529 mL | 4.8821 mL | |
| 15 mM | 0.1302 mL | 0.6510 mL | 1.3019 mL | 3.2548 mL | |
| 20 mM | 0.0976 mL | 0.4882 mL | 0.9764 mL | 2.4411 mL | |
| 25 mM | 0.0781 mL | 0.3906 mL | 0.7811 mL | 1.9529 mL | |
| 30 mM | 0.0651 mL | 0.3255 mL | 0.6510 mL | 1.6274 mL | |
| 40 mM | 0.0488 mL | 0.2441 mL | 0.4882 mL | 1.2205 mL | |
| 50 mM | 0.0391 mL | 0.1953 mL | 0.3906 mL | 0.9764 mL | |
| 60 mM | 0.0325 mL | 0.1627 mL | 0.3255 mL | 0.8137 mL | |
| 80 mM | 0.0244 mL | 0.1221 mL | 0.2441 mL | 0.6103 mL | |
| 100 mM | 0.0195 mL | 0.0976 mL | 0.1953 mL | 0.4882 mL |
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