JNJ-5207787 | CAS#683746-68-1 | Y2 Receptor Antagonist |MedKoo

JNJ-5207787
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 531989

CAS#: 683746-68-1

Description: JNJ-5207787 is a small molecule antagonist of the neuropeptide Y Y2 receptor.

Chemical Structure

JNJ-5207787

CAS# 683746-68-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 531989
Name: JNJ-5207787
CAS#: 683746-68-1
Chemical Formula: C32H38N4O2
Exact Mass: 510.30
Molecular Weight: 510.682
Elemental Analysis: C, 75.26; H, 7.50; N, 10.97; O, 6.27

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 550	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: JNJ-5207787; JNJ 5207787; JNJ5207787.

IUPAC/Chemical Name: (E)-N-(1-acetyl-2,3-dihydroindol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide

InChi Key: DSEJCLDJIFTPPH-FMIVXFBMSA-N

InChi Code: InChI=1S/C32H38N4O2/c1-24(37)35-20-14-28-10-11-30(22-31(28)35)36(32(38)12-9-26-7-4-8-27(21-26)23-33)29-15-18-34(19-16-29)17-13-25-5-2-3-6-25/h4,7-12,21-22,25,29H,2-3,5-6,13-20H2,1H3/b12-9+

SMILES Code: O=C(N(C1=CC2=C(C=C1)CCN2C(C)=O)C3CCN(CCC4CCCC4)CC3)/C=C/C5=CC=CC(C#N)=C5

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: >2 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:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	JNJ-5207787 is a small molecule antagonist of the neuropeptide Y Y2 receptor.
In vitro activity:	JNJ-5207787 inhibited the binding of peptide YY (PYY) to human Y(2) receptor in KAN-Ts cells (pIC(50) = 7.00 +/- 0.10) and to rat Y(2) receptors in rat hippocampus (pIC(50) = 7.10 +/- 0.20). Reference: J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. https://pubmed.ncbi.nlm.nih.gov/14617685/
In vivo activity:	When this study injected JNJ 5207787 together with PTZ (either dose) the number of seizures, however, became significantly increased. Injection of the Y2 receptor antagonist JNJ 5207787 prevents this protective action of NPY only when release of the peptide is triggered by injection of PTZ and induces pronounced convulsions. Reference: Front Mol Neurosci. 2022 Oct 13;15:974784. https://pubmed.ncbi.nlm.nih.gov/36311021/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	5.1	10.01
	Ethanol	5.1	10.01

Preparing Stock Solutions

The following data is based on the product molecular weight 510.68 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	1.15 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:	1. Bonaventure P, Nepomuceno D, Mazur C, Lord B, Rudolph DA, Jablonowski JA, Carruthers NI, Lovenberg TW. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. doi: 10.1124/jpet.103.060459. Epub 2003 Nov 14. PMID: 14617685. 2. Jablonowski JA, Chai W, Li X, Rudolph DA, Murray WV, Youngman MA, Dax SL, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI. Novel non-peptidic neuropeptide Y Y2 receptor antagonists. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1239-42. doi: 10.1016/j.bmcl.2003.12.057. PMID: 14980673. 3. Drexel M, Sperk G. Seizure-induced overexpression of NPY induces epileptic tolerance in a mouse model of spontaneous recurrent seizures. Front Mol Neurosci. 2022 Oct 13;15:974784. doi: 10.3389/fnmol.2022.974784. PMID: 36311021; PMCID: PMC9608171.
In vitro protocol:	1. Bonaventure P, Nepomuceno D, Mazur C, Lord B, Rudolph DA, Jablonowski JA, Carruthers NI, Lovenberg TW. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. doi: 10.1124/jpet.103.060459. Epub 2003 Nov 14. PMID: 14617685. 2. Jablonowski JA, Chai W, Li X, Rudolph DA, Murray WV, Youngman MA, Dax SL, Nepomuceno D, Bonaventure P, Lovenberg TW, Carruthers NI. Novel non-peptidic neuropeptide Y Y2 receptor antagonists. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1239-42. doi: 10.1016/j.bmcl.2003.12.057. PMID: 14980673.
In vivo protocol:	1. Drexel M, Sperk G. Seizure-induced overexpression of NPY induces epileptic tolerance in a mouse model of spontaneous recurrent seizures. Front Mol Neurosci. 2022 Oct 13;15:974784. doi: 10.3389/fnmol.2022.974784. PMID: 36311021; PMCID: PMC9608171. 2. Bonaventure P, Nepomuceno D, Mazur C, Lord B, Rudolph DA, Jablonowski JA, Carruthers NI, Lovenberg TW. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-ethyl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. doi: 10.1124/jpet.103.060459. Epub 2003 Nov 14. PMID: 14617685.

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1: Mittapalli GK, Roberts E. Ligands of the neuropeptide Y Y2 receptor. Bioorg Med Chem Lett. 2014 Jan 15;24(2):430-41. doi: 10.1016/j.bmcl.2013.11.061. Review. PubMed PMID: 24365162; PubMed Central PMCID: PMC4672871.

2: Bonaventure P, Nepomuceno D, Mazur C, Lord B, Rudolph DA, Jablonowski JA, Carruthers NI, Lovenberg TW. Characterization of N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyano-phenyl)-N-[1-(2-cyclopentyl-eth yl)-piperidin-4yl]acrylamide (JNJ-5207787), a small molecule antagonist of the neuropeptide Y Y2 receptor. J Pharmacol Exp Ther. 2004 Mar;308(3):1130-7. PubMed PMID: 14617685.

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