
Biological Activity
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
CGP 71683 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 512.07 |
Formula | C26H29N5O2S.HCl |
Storage | Desiccate at +4°C |
Purity | ≥99% (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.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 51.21 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 512.07. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
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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