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(2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide, also known as JNJ-5207787, is a small molecule antagonist of the neuropeptide Y (NPY) receptor Y2. It effectively blocks peptide YY binding with an IC50 of 100 nM and exhibits 100-fold selectivity for Y2 over other NPY receptors. JNJ-5207787 demonstrates intraperitoneal bioavailability and brain penetration in rats, with the ability to occupy up to 50% of Y2 receptor binding sites in the hypothalamic area. Its minimal effect on a panel of 50 receptors, ion channels, and transporters, except for sodium channel 2, highlights its potential as a selective therapeutic agent.

683746-68-1

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  • (2E)-N-(1-Acetyl-2,3-dihydro-1H-indol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)-4-piperidinyl]-2-propenamide

    Cas No: 683746-68-1

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  • (E)-N-(1-acetyl-2,3-dihydroindol-6-yl)-3-(3-cyanophenyl)-N-[1-(2-cyclopentylethyl)piperidin-4-yl]prop-2-enamide

    Cas No: 683746-68-1

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683746-68-1 Usage

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Used in Pharmaceutical Industry:
JNJ-5207787 is utilized as a small molecule antagonist for the neuropeptide Y Y2 receptor, playing a crucial role in the development of therapeutic agents targeting the NPY system. Its high selectivity and brain penetration make it a promising candidate for treating various central nervous system disorders, including obesity, anxiety, and depression, by modulating the NPY signaling pathway.
Used in Research Applications:
In the field of scientific research, JNJ-5207787 serves as a valuable tool for studying the role of the NPY Y2 receptor in physiological and pathological processes. Its use in experimental models helps researchers to better understand the mechanisms underlying NPY-mediated effects and to identify potential therapeutic targets for the development of novel treatments.

Check Digit Verification of cas no

The CAS Registry Mumber 683746-68-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,8,3,7,4 and 6 respectively; the second part has 2 digits, 6 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 683746-68:
(8*6)+(7*8)+(6*3)+(5*7)+(4*4)+(3*6)+(2*6)+(1*8)=211
211 % 10 = 1
So 683746-68-1 is a valid CAS Registry Number.

683746-68-1Downstream Products

683746-68-1Relevant articles and documents

Expedient reductive animation of aldehyde bisulfite adducts

Pandit, Chennagiri R.,Mani, Neelakandha S.

scheme or table, p. 4032 - 4036 (2010/03/24)

A novel, one-pot protocol for the direct reductive animation of aldehyde bisulfite adducts is reported. Bisulfite adducts of aliphatic and aromatic aldehydes, on treatment with an organic base under non-aqueous conditions liberate the aldehyde in situ, which then undergoes efficient reductive amination with amines in the presence of sodium triacetoxyborohydride.

Non-peptidic NPY Y2 receptor inhibitors

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Page/Page column 26, (2010/02/11)

The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

Novel non-peptidic neuropeptide Y Y2 receptor antagonists

Jablonowski, Jill A.,Chai, Wenying,Li, Xiaobing,Rudolph, Dale A.,Murray, William V.,Youngman, Mark A.,Dax, Scott L.,Nepomuceno, Diane,Bonaventure, Pascal,Lovenberg, Timothy W.,Carruthers, Nicholas I.

, p. 1239 - 1242 (2007/10/03)

Through SAR studies of a piperidinylindoline cinnamide HTS lead, the first potent, non-peptide, low molecular weight selective Neuropeptide Y Y 2 (NPY Y2) antagonists have been synthesized. The SAR studies around the piperidinyl, the indolinyl, and the cinnamyl moieties are discussed.

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