Formulation: A solid
Formal Name: 4-[(3R)-3-amino-1-pyrrolidinyl]-6-(1-methylethyl)-2-pyrimidinamine
Purity: ≥98%
Formula Markup: C11H19N5
Formula Weight: 221,3
Shelf life (days): 1460
CAS Number: 1046447-90-8
Notes: JNJ-39758979 is a histamine H4 receptor antagonist (Ki = 12.5 nM for the human receptor).{49876} 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 (Item No. 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; Item No. 33264) and inhibits histamine-induced pruritis in mice.{49876,49877} 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.{49878}
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