JNJ10191584 maleate
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 869497-75-6
- Formula: C17H19ClN4O5
- Molecular Weight:394.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Histamine Receptor Isoforms
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Biological Activity
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Human H4 Receptor 26 nM (Ki) |
human H3 receptor 14.1 μM (Ki) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 869497-75-6
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Molecular Weight 394.81
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Formula C17H19ClN4O5
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SMILES
OC(/C=C\C(O)=O)=O.O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2
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Synonyms
VUF6002 maleate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (270 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)