CGP 71683 hydrochloride (Synonyms: CGP 71683A) |
| Katalog-Nr.GC10167 |
CGP 71683-Hydrochlorid ist ein kompetitiver Neuropeptid-Y5-Rezeptorantagonist mit einem Ki von 1,3 nM und zeigt keine offensichtliche Aktivität am Y1-Rezeptor (Ki, \u003e4000 nM) und am Y2-Rezeptor (Ki, 200 nM) in Zellmembranen.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 192322-50-2
Sample solution is provided at 25 µL, 10mM.
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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.
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].
CGP71683 (15 nmol/rat, icv, twice daily) shows anorexigenic effect, reducing food intake and bady weight of fed rats. CGP71683 causes 3-times higher serum total T4 and 37% increase in free T4 in the fasted rats than in the fasted controls rats[2].
Reference:
[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.
[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.
Animal experiment: | 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]. |
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. | |
| Cas No. | 192322-50-2 | SDF | |
| Überlieferungen | CGP 71683A | ||
| Chemical Name | N-(((1r,4r)-4-(((4-aminoquinazolin-2-yl)amino)methyl)cyclohexyl)methyl)naphthalene-1-sulfonamide hydrochloride | ||
| Canonical SMILES | O=S(NC[C@@H]1CC[C@@H](CNC2=NC(N)=C3C(C=CC=C3)=N2)CC1)(C4=CC=CC5=CC=CC=C45)=O.Cl | ||
| Formula | C26H29N5O2S.HCl | M.Wt | 512.07 |
| Löslichkeit | <51.21mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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