Molecular Formula | C26H30ClN5O2S |
Molar Mass | 512.07 |
Solubility | DMSO: 120 mg/mL (234.34 mM)Water: 10 mg/mL (19.53 mM)( < 1 mg/ml refers to the product slightly soluble or insoluble) |
Appearance | solid |
Color | off-white |
Storage Condition | Inert atmosphere,2-8°C |
Use | CGP71683 hydrochloride is a competitive neuropeptide receptor (neuropeptide Y5 receptor) antagonist with a Ki value of 1.3 nM. In cell membrane, it has no obvious effect on Y1 and Y2 receptors (Ki,>4000 nM,200 nM). |
In vitro study | CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a K i of 1.3 nM, and shows no obvious activity at Y1 receptor (K i , >4000 nM) and Y2 receptor (K i , 200 nM) in cell membranes. |
In vivo study | 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. |
Safety Description | 24/25 - Avoid contact with skin and eyes. |
WGK Germany | 3 |
Reference Show more | 1: Ghahramanian Golzar M, Babri S, Ataie Z, Ebrahimi H, Mirzaie F, Mohaddes G. NPY Receptors Blockade Prevents Anticonvulsant Action of Ghrelin in the Hippocampus of Rat. Adv Pharm Bull. 2013;3(2):265-71. doi: 10.5681/apb.2013.043. Epub 2013 Aug 20. PubMed PMID: 24312846; PubMed Central PMCID: PMC3848244. 2: Li L, Mayer M, Schneider E, Schreiber E, Bernhardt G, Peng S, Buschauer A. Preparation of fluorescent nonpeptidic neuropeptide Y receptor ligands: analogues of the quinazoline-type anti-obesity Y5 antagonist CGP 71683A. Arch Pharm (Weinheim). 2003 Dec;336(12):585-90. PubMed PMID: 14677152. 3: Lecklin A, Lundell I, Paananen L, Wikberg JE, Männistö PT, Larhammar D. Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br J Pharmacol. 2002 Apr;135(8):2029-37. PubMed PMID: 11959807; PubMed Central PMCID: PMC1573328. 4: Della Zuana O, Sadlo M, Germain M, Félétou M, Chamorro S, Tisserand F, de Montrion C, Boivin JF, Duhault J, Boutin JA, Levens N. Reduced food intake in response to CGP 71683A may be due to mechanisms other than NPY Y5 receptor blockade. Int J Obes Relat Metab Disord. 2001 Jan;25(1):84-94. PubMed PMID: 11244462. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.953 ml | 9.764 ml | 19.529 ml |
5 mM | 0.391 ml | 1.953 ml | 3.906 ml |
10 mM | 0.195 ml | 0.976 ml | 1.953 ml |
5 mM | 0.039 ml | 0.195 ml | 0.391 ml |