JNJ10191584 maleate  (Synonyms: VUF6002 maleate)

JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H₄ receptor antagonist with a K_i value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H₄ receptor over the H₃ receptor with a K_i value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively^[1][2].

JNJ10191584 maleate shows binding affinity of 26 nM and 14.1 μM to H₄ and H₃ receptor, respectively^[1].
JNJ10191584 maleate (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ10191584 maleate (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice^[1].
JNJ10191584 maleate (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice^[1].
JNJ10191584 maleate (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

394.81

C₁₇H₁₉ClN₄O₅

869497-75-6

OC(/C=C\C(O)=O)=O.O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]