JNJ-31020028

• CAT Number: I000400
• CAS Number: 1094873-14-9
• Molecular Formula: C₃₄H₃₆FN₅O₂
• Molecular Weight: 565.68
• Purity: ≥95%
• Target: Neuroscience Peptides
• Solubility: DMSO: ≤ 21.5 mg/mL
• Storage: Store at -20°C
• IC50: 8.07/8.22(human/rat pIC50) [1]
• InChI: InChI=1S/C34H36FN5O2/c1-3-38(4-2)34(42)32(25-11-6-5-7-12-25)40-21-19-39(20-22-40)31-17-16-27(23-30(31)35)37-33(41)29-15-9-8-14-28(29)26-13-10-18-36-24-26/h5-18,23-24,32H,3-4,19-22H2,1-2H3,(H,37,41)
• InChIKey: OVUNRYUVDVWTTE-UHFFFAOYSA-N
• SMILES: CCN(CC)C(=O)C(C1=CC=CC=C1)N2CCN(CC2)C3=C(C=C(C=C3)NC(=O)C4=CC=CC=C4C5=CN=CC=C5)F

JNJ-31020028(CAT: I000400) is a chemical compound with potential analgesic and anti-inflammatory properties. It acts as a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) ion channel. By blocking TRPV1, JNJ-31020028 inhibits the transmission of pain signals and reduces neurogenic inflammation. It has been investigated for its potential use in the treatment of various pain conditions, including neuropathic pain and inflammatory pain. JNJ-31020028 represents a promising target for the development of novel therapeutics aimed at modulating TRPV1-mediated pain pathways.

Reference

1:PET brain imaging of neuropeptide Y2 receptors using N-11C-methyl-JNJ-31020028 in pigs. Winterdahl M, Audrain H, Landau AM, Smith DF, Bonaventure P, Shoblock JR, Carruthers N, Swanson D, Bender D.J Nucl Med. 2014 Apr;55(4):635-9. doi: 10.2967/jnumed.113.125351. Epub 2014 Mar 10. PMID: 24614224 Free Article2:Chronic administration of the Y2 receptor antagonist, JNJ-31020028, induced anti-depressant like-behaviors in olfactory bulbectomized rat. Morales-Medina JC, Dumont Y, Bonaventure P, Quirion R.Neuropeptides. 2012 Dec;46(6):329-34. doi: 10.1016/j.npep.2012.09.009. Epub 2012 Oct 25. PMID: 23103057 3:The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y₂ receptor. Swanson DM, Wong VD, Jablonowski JA, Shah C, Rudolph DA, Dvorak CA, Seierstad M, Dvorak LK, Morton K, Nepomuceno D, Atack JR, Bonaventure P, Lovenberg TW, Carruthers NI.Bioorg Med Chem Lett. 2011 Sep 15;21(18):5552-6. doi: 10.1016/j.bmcl.2011.06.136. Epub 2011 Jul 18. PMID: 21802951 4:Effects of a selective Y2R antagonist, JNJ-31020028, on nicotine abstinence-related social anxiety-like behavior, neuropeptide Y and corticotropin releasing factor mRNA levels in the novelty-seeking phenotype. Aydin C, Oztan O, Isgor C.Behav Brain Res. 2011 Sep 23;222(2):332-41. doi: 10.1016/j.bbr.2011.03.067. Epub 2011 Apr 8. PMID: 21497168 Free PMC Article5:The novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist, JNJ-31020028, tested in animal models of alcohol consumption, relapse, and anxiety. Cippitelli A, Rezvani AH, Robinson JE, Eisenberg L, Levin ED, Bonaventure P, Motley ST, Lovenberg TW, Heilig M, Thorsell A.Alcohol. 2011 Sep;45(6):567-76. doi: 10.1016/j.alcohol.2010.09.003. Epub 2010 Dec 10. PMID: 21145691 6:In vitro and in vivo characterization of JNJ-31020028 (N-(4-{4-[2-(diethylamino)-2-oxo-1-phenylethyl]piperazin-1-yl}-3-fluorophenyl)-2-pyridin-3-ylbenzamide), a selective brain penetrant small molecule antagonist of the neuropeptide Y Y(2) receptor. Shoblock JR, Welty N, Nepomuceno D, Lord B, Aluisio L, Fraser I, Motley ST, Sutton SW, Morton K, Galici R, Atack JR, Dvorak L, Swanson DM, Carruthers NI, Dvorak C, Lovenberg TW, Bonaventure P.Psychopharmacology (Berl). 2010 Feb;208(2):265-77. doi: 10.1007/s00213-009-1726-x. Epub 2009 Dec 2. PMID: 19953226