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Submit ReviewCGP 71683 hydrochloride
Description: Highly selective and potent non-peptide NPY Y5 receptor antagonist
Chemical Name: N-[[trans-4-[[(4-Amino-2-quinazolinyl)amino]methyl]cyclohexyl]methyl]-1-naphthalenesulfonamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for CGP 71683 hydrochloride
CGP 71683 hydrochloride is an extremely selective, non-peptide NPY Y5 receptor antagonist. Displays > 1000-fold selectivity over Y1, Y2 and Y4 receptors; IC50 values are 1.4, 2765, 7187 and 5637 nM at cloned rat Y5, Y1, Y2 and Y4 receptors respectively. Potently inhibits NPY-induced food intake following i.p. administration in diabetic, free-feeding and fasted rats.
Compound Libraries for CGP 71683 hydrochloride
CGP 71683 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for CGP 71683 hydrochloride
| M. Wt | 512.07 |
| Formula | C26H29N5O2S.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 192322-50-2 |
| PubChem ID | 9849276 |
| InChI Key | DIQDKUNCSVFGHH-UHFFFAOYSA-N |
| Smiles | NC1=NC(NC[C@H]3CC[C@H](CNS(=O)(C4=CC=CC5=C4C=CC=C5)=O)CC3)=NC2=C1C=CC=C2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CGP 71683 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.21 | 100 |
Preparing Stock Solutions for CGP 71683 hydrochloride
The following data is based on the product molecular weight 512.07. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.95 mL | 9.76 mL | 19.53 mL |
| 5 mM | 0.39 mL | 1.95 mL | 3.91 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.95 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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Product Datasheets for CGP 71683 hydrochloride
References for CGP 71683 hydrochloride
References are publications that support the biological activity of the product.
Criscione et al (1998) Food intake in free-feeding and energy-deprived lean rats is mediated by the neuropeptide Y5 receptor. J.Clin.Invest. 102 2136 PMID: 9854049
Dumont et al (2000) Potent and selective tools to investigate neuropeptide Y receptors in the central and peripheral nervous systems: BIB03304 (Y1) and CGP71683A (Y5). Can.J.Physiol.Pharmacol. 78 116 PMID: 10737674
Lecklin et al (2002) Receptor subtypes Y1 and Y5 mediate neuropeptide Y induced feeding in the guinea-pig. Br.J.Pharmacol. 135 2029 PMID: 11959807
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Keywords: CGP 71683 hydrochloride, CGP 71683 hydrochloride supplier, selective, potent, non-peptide, NPY, Y5, receptor, antagonists, Neuropeptide, Y, Receptors, CGP71683, hydrochloride, neuropeptides, 2199, Tocris Bioscience
6 Citations for CGP 71683 hydrochloride
Citations are publications that use Tocris products. Selected citations for CGP 71683 hydrochloride include:
Demorrow et al (2011) Neuropeptide Y inhibits cholangiocarcinoma cell growth and invasion. Nature 300 C1078 PMID: 21270292
Lu et al (2011) Dipeptidyl peptidases as survival factors in Ewing sarcoma family of tumors: implications for tumor biology and therapy. J Biol Chem 286 27494 PMID: 21680731
Tilan et al (2013) Hypoxia shifts activity of neuropeptide Y in Ewing sarcoma from growth-inhibitory to growth-promoting effects. Oncotarget 4 2487 PMID: 24318733
Reidelberger et al (2013) Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats. Am J Physiol Endocrinol Metab 304 E944 PMID: 23482449
Han et al (2012) Stress hormone epinephrine enhances adipogenesis in murine embryonic stem cells by up-regulating the neuropeptide Y system. PLoS One 7 e36609 PMID: 22570731
Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Am J Physiol Cell Physiol 488 172 PMID: 22801496
Do you know of a great paper that uses CGP 71683 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.