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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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CGP 71683A, a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, is a potent and highly selective non-peptide antagonist of the NPY Y(5) receptor in the study of obesity.
| Targets |
Y5 receptor ( Ki = 1.3 nM ); Y2 receptor ( Ki = 200 nM ); Y1 receptor ( Ki > 4000 nM )
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|---|---|
| ln Vitro |
CGP71683 hydrochloride is a competitive antagonist of neuropeptide Y5 receptor with a Ki of 1.3 nM. It exhibits no discernible activity at the Y1 receptor (Ki, >4000 nM) or the Y2 receptor (Ki, 200 nM) in membranes of cells[1].
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| ln Vivo |
CGP71683 (15 nmol/rat, icv, twice daily) exhibits anorexigenic effects, lowering fed rats' body weight and food intake. CGP71683 results in three times higher serum total T4 and a 37% increase in free T4 levels compared to the fasted control rats[2].
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| Animal Protocol |
Rats: CGP71683 is dissolved in 30% DMSO and, prior to the experiment, stored frozen at -20°C. Every microinjection comprises 2 microliters of either 30% DMSO vehicle or CGP71683 (7.5 nmol/μL; 15 nmol/rat) injected via the guide cannula over a 30- to 60-second period, adhering to the following protocols: I-Rats given free access to chow are given six microinjections (15 nmol/rat, spaced 10–14 hours apart) and are killed one hour after the final injection, which occurs between 9 and 10 a.m. The amount of food consumed is calculated by calculating the daily reduction in chow mass (g) right before each intravenous injection. II: After fasting for 72 hours, rats are given a single microinjection of either vehicle or CGP71683 (15 nmol/rat) and are then killed one hour later. III - Rats are given multiple injections of vehicle or CGP71683 over the course of a 72-hour fast, following the same protocol as fed animals. The fasting period began 10 hours prior to the first microinjection. Rats are decapitated at the conclusion of the experiments, and serum is extracted from the trunk blood to measure the hormone concentrations[2].
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| References |
| Molecular Formula |
C26H30CLN5O2S
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|---|---|
| Molecular Weight |
512.07
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| Exact Mass |
511.18
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| Elemental Analysis |
C, 60.98; H, 5.91; Cl, 6.92; N, 13.68; O, 6.25; S, 6.26
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| CAS # |
192322-50-2
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| Related CAS # |
192321-23-6; 192322-50-2 (HCl)
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| Appearance |
Solid powder
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| SMILES |
C1CC(CCC1CNC2=NC3=CC=CC=C3C(=N2)N)CNS(=O)(=O)C4=CC=CC5=CC=CC=C54.Cl
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| InChi Key |
DIQDKUNCSVFGHH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H29N5O2S.ClH/c27-25-22-9-3-4-10-23(22)30-26(31-25)28-16-18-12-14-19(15-13-18)17-29-34(32,33)24-11-5-7-20-6-1-2-8-21(20)24;/h1-11,18-19,29H,12-17H2,(H3,27,28,30,31);1H
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| Chemical Name |
N-[[4-[[(4-aminoquinazolin-2-yl)amino]methyl]cyclohexyl]methyl]naphthalene-1-sulfonamide;hydrochloride
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| Synonyms |
CGP-71683A HCl; CGP71683A; CGP-71683A; CGP 71683A
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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 |
| 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) |
DMSO: 100~160 mg/mL (195.3~312.5 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.67 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.67 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.67 mg/mL (5.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9529 mL | 9.7643 mL | 19.5286 mL | |
| 5 mM | 0.3906 mL | 1.9529 mL | 3.9057 mL | |
| 10 mM | 0.1953 mL | 0.9764 mL | 1.9529 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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