JNJ-39758979

JNJ-39758979 is a histamine H4 receptor antagonist (Ki = 12.5 nM for the human receptor). It is selective for the histamine H4 receptor over histamine H1, H2, and H3 receptors (Kis = >1,000, >1,000, and 1,043 nM, respectively, for the human receptors), as well as 48 other receptors, ion channels, and transporters at 1 µM and 66 kinases at 10 µM. JNJ-39758979 inhibits chemotaxis induced by histamine (Cay-33828) in isolated mouse bone marrow-derived mast cells (IC50 = 8 nM). It reduces ovalbumin-induced eosinophil infiltration in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of asthma when administered at doses ranging from 0.2 to 20 mg/kg. JNJ-39758979 (20 mg/kg) decreases ear edema in a mouse model of Th2-dependent contact hypersensitivity induced by fluorescein isothiocyanate (FITC, Cay-33264) and inhibits histamine-induced pruritis in mice. It also reduces nephropathy, but does not affect body weight or blood glucose levels, in a mouse model of streptozotocin-induced diabetes when administered at a dose of 100 mg/kg.Formal Name: 4-[(3R)-3-amino-1-pyrrolidinyl]-6-(1-methylethyl)-2-pyrimidinamine. CAS Number: 1046447-90-8. Molecular Formula: C11H19N5. Formula Weight: 221.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml. SMILES: CC(C1=CC(N2C[C@H](N)CC2)=NC(N)=N1)C. InChi Code: InChI=1S/C11H19N5/c1-7(2)9-5-10(15-11(13)14-9)16-4-3-8(12)6-16/h5,7-8H,3-4,6,12H2,1-2H3,(H2,13,14,15)/t8-/m1/s1. InChi Key: COOGVHJHSCBOQT-MRVPVSSYSA-N.