CGP 71683 (free base)

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MedKoo CAT#: 412732

CAS#: 192321-23-6 (free base)

Description: CGP 71683 (free base) is a potent and highly selective non-peptide antagonist of the NPY Y(5) receptor in the study of obesity.

Chemical Structure

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CGP 71683 (free base)
CAS# 192321-23-6 (free base)
Instruction

Theoretical Analysis

MedKoo Cat#: 412732
Name: CGP 71683 (free base)
CAS#: 192321-23-6 (free base)
Chemical Formula: C26H29N5O2S
Exact Mass: 475.20
Molecular Weight: 475.610
Elemental Analysis: C, 65.66; H, 6.15; N, 14.73; O, 6.73; S, 6.74

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 192321-23-6 (free base)   192322-50-2 (HCl)    

Synonym: CGP 71683 (free base)

IUPAC/Chemical Name: N-(((1r,4r)-4-(((4-aminoquinazolin-2-yl)amino)methyl)cyclohexyl)methyl)naphthalene-1-sulfonamide

InChi Key: UULIGRNKXHCLQN-WGSAOQKQSA-N

InChi Code: InChI=1S/C26H29N5O2S/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)/t18-,19-

SMILES Code: Nc(nc(NC[C@@H]1CC[C@H](CC1)CNS(=O)(c(ccc2)c3c2cccc3)=O)n4)c5c4cccc5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 475.61 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Kermani M, Eliassi A. Gastric acid secretion induced by paraventricular nucleus microinjection of orexin A is mediated through activation of neuropeptide Yergic system. Neuroscience. 2012 Dec 13;226:81-8. doi: 10.1016/j.neuroscience.2012.08.052. Epub 2012 Sep 15. PMID: 22986171.

2: Reidelberger R, Haver A, Chelikani PK. Role of peptide YY(3-36) in the satiety produced by gastric delivery of macronutrients in rats. Am J Physiol Endocrinol Metab. 2013 May 1;304(9):E944-50. doi: 10.1152/ajpendo.00075.2013. Epub 2013 Mar 12. PMID: 23482449; PMCID: PMC3651646.

3: 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. doi: 10.1038/sj.ijo.0801472. PMID: 11244462.

4: Eltahan HM, Bahry MA, Yang H, Han G, Nguyen LTN, Ikeda H, Ali MN, Amber KA, Furuse M, Chowdhury VS. Central NPY-Y5 sub-receptor partially functions as a mediator of NPY-induced hypothermia and affords thermotolerance in heat-exposed fasted chicks. Physiol Rep. 2017 Dec;5(23):e13511. doi: 10.14814/phy2.13511. PMID: 29208684; PMCID: PMC5727273.

5: Chamorro S, Della-Zuana O, Fauchère JL, Félétou M, Galizzi JP, Levens N. Appetite suppression based on selective inhibition of NPY receptors. Int J Obes Relat Metab Disord. 2002 Mar;26(3):281-98. doi: 10.1038/sj.ijo.0801948. PMID: 11896483.

6: Criscione L, Rigollier P, Batzl-Hartmann C, Rüeger H, Stricker-Krongrad A, Wyss P, Brunner L, Whitebread S, Yamaguchi Y, Gerald C, Heurich RO, Walker MW, Chiesi M, Schilling W, Hofbauer KG, Levens N. Food intake in free-feeding and energy-deprived lean rats is mediated by the neuropeptide Y5 receptor. J Clin Invest. 1998 Dec 15;102(12):2136-45. doi: 10.1172/JCI4188. PMID: 9854049; PMCID: PMC509168.

7: 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. doi: 10.1002/ardp.200300813. PMID: 14677152.

8: Costa-e-Sousa RH, Souza LL, Calviño C, Cabanelas A, Almeida NA, Oliveira KJ, Pazos-Moura CC. 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. doi: 10.1016/j.regpep.2011.07.001. Epub 2011 Jul 21. PMID: 21771616.

9: Félétou M, Nicolas JP, Rodriguez M, Beauverger P, Galizzi JP, Boutin JA, Duhault J. NPY receptor subtype in the rabbit isolated ileum. Br J Pharmacol. 1999 Jun;127(3):795-801. doi: 10.1038/sj.bjp.0702594. PMID: 10401572; PMCID: PMC1566062.

10: King PJ, Widdowson PS, Doods HN, Williams G. Regulation of neuropeptide Y release by neuropeptide Y receptor ligands and calcium channel antagonists in hypothalamic slices. J Neurochem. 1999 Aug;73(2):641-6. doi: 10.1046/j.1471-4159.1999.0730641.x. PMID: 10428060.