JNJ10191584JNJ10191584
MedChemExpress (MCE)
HY-123532
73903-17-0
VUF6002
99.95%
4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months
-20°C, 1 month (protect from light, stored under nitrogen)
Room temperature in continental US
may vary elsewhere.
JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
JNJ10191584 shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively[1]. JNJ10191584 (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1].
JNJ10191584 (10 μg/μL
intra locus coeruleus (LC) administration
once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1]. JNJ10191584 (10 μg/μL
intra LC administration
once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1]. JNJ10191584 (6 μg/mouse
intrathecal administration
pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].
Human H4 Receptor 26 nM (Ki) human H3 receptor 14.1 μM (Ki)
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[1]. Venable JD, et al. Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists. J Med Chem. 2005 Dec 29
48(26):8289-98. [Content Brief]
[2]. Sanna MD, et al. Histamine H4 receptor stimulation in the locus coeruleus attenuates neuropathic pain by promoting the coeruleospinal noradrenergic inhibitory pathway. Eur J Pharmacol. 2020 Feb 5
868:172859. [Content Brief]