INCB38579

• CAT Number: I042975
• CAS Number: 1246207-65-7
• Molecular Formula: C25H34N6O
• Molecular Weight: 434.58
• Purity: ≥95%
• Synonyms: 1-[7-[2-amino-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl]-3,4-dihydro-1H-isoquinolin-2-yl]-2-cyclopentylethanone
• InChI: InChI=1S/C25H34N6O/c1-29-10-12-30(13-11-29)23-16-22(27-25(26)28-23)20-7-6-19-8-9-31(17-21(19)15-20)24(32)14-18-4-2-3-5-18/h6-7,15-16,18H,2-5,8-14,17H2,1H3,(H2,26,27,28)
• InChIKey: LZOCXAJJOQPLKB-UHFFFAOYSA-N
• SMILES: CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC4=C(CCN(C4)C(=O)CC5CCCC5)C=C3)N

INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].
INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4 receptors[1].
INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells[1].
NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently[1].
INCB38579 (oral gavage; 100 mg/kg; once) inhibits histamine-mediated pruritus in mice[1].
INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain[1].
INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice[1].

Reference

[1]. Niu Shin, et al. INCB38579, a novel and potent histamine H₄ receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56.
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