JNJ 10191584 maleate 是一种具有口服活性的选择性 H4 受体拮抗剂 (Ki = 26 nM)。 JNJ 10191584 maleate 抑制嗜酸性粒细胞和肥大细胞的趋化性(IC50 = 530 nM 和 138 nM)。
产品描述
JNJ 10191584 maleate is an orally active and selective antagonist of H4 receptor (Ki = 26 nM). JNJ 10191584 maleate inhibits chemotaxis of eosinophils and mast cells (IC50 = 530 nM and 138 nM).
体外活性
JNJ 10191584 maleate shows 540-fold selectivity to H4 receptor(Ki = 14.1 μM)[2].
体内活性
In spared nerve injury mice, JNJ 10191584 maleate (10 μg/μL; intra locus coeruleus administration) abolishes VUF-induced anti-allodynic effect and prevents the anti-allodynic effect of VUF 8430. JNJ 10191584 maleate (6 μg/mouse; intrathecal administration) prevents VUF 8430-induced anti-allodynic effect[2].
Cas No.
869497-75-6
分子式
C17H19ClN4O5
分子量
394.81
别名
JNJ 10191584 maleate salt;VUF6002 maleate
储存和溶解度
DMSO:18mg/mL (45.6mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years