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JNJ10191584

Cat. No. M30560
JNJ10191584 Structure
Synonym:

VUF6002

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Biological Activity

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.

Chemical Information
Molecular Weight 278.74
Formula C13H15ClN4O
CAS Number 73903-17-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Marek Grosicki, et al. Eur J Pharmacol. Eosinophils adhesion assay as a tool for phenotypic drug screening - The pharmacology of 1,3,5 - Triazine and 1H-indole like derivatives against the human histamine H4 receptor

[2] Mizuki Watanabe, et al. Bioorg Med Chem Lett. Design and synthesis of histamine H3/H4 receptor ligands with a cyclopropane scaffold

[3] Satoshi Tanaka, et al. Biochem Biophys Res Commun. Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines

[4] J P Prestifilippo, et al. Oral Dis. Pharmacological targeting of histamine H4 receptor in periodontal disease

[5] Ondrej Vasicek, et al. Life Sci. Role of histamine receptors in the effects of histamine on the production of reactive oxygen species by whole blood phagocytes

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Keywords: JNJ10191584, VUF6002 supplier, Histamine Receptor, inhibitors, activators

 
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