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

MedKoo Cat#: 531989 | Name: JNJ-5207787

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Description:

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

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

Chemical Structure

JNJ-5207787

CAS#683746-68-1

Theoretical Analysis

MedKoo Cat#: 531989

Name: JNJ-5207787

CAS#: 683746-68-1

Chemical Formula: C32H38N4O2

Exact Mass: 510.2995

Molecular Weight: 510.68

Elemental Analysis: C, 75.26; H, 7.50; N, 10.97; O, 6.27

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 550.00	2 Weeks

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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/

	Solvent	mg/mL	mM
Solubility
	DMSO	5.1	10.01
	Ethanol	5.1	10.01

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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:

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.

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.