PF-3893787 hydrochloride (Synonyms: PF-3893787 hydrochloride) |
Catalog No.GC31790 |
PF-3893787 염산염(PF-3893787 염산염)은 새로운 히스타민 H4 수용체 길항제 결합 친화도(Ki=2.4nM)이며 기능적(Ki=1.56nM) 길항제이기도 합니다.
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Cas No.: 2096455-90-0
Sample solution is provided at 25 µL, 10mM.
PF-3893787 hydrochloride is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
PF-3893787 is tested and observed binding Ki=2.4 nM and functional Ki=1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and PF-3893787 (Compound 13) is fast on/fast off on rhH4R. The in vitro IC50 on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC50 for >90% receptor occupancy (and therefore near complete inhibition of the response) suggested a concentration of 12 nM. The data in the whole blood GAFS assay demonstrates that the imetit induced shape change is completely blocked at a total blood concentration of 30 nM (which correcting for PPB and blood partitioning equates to approximately 10 nM free). For the purpose of dose projection and safety margin calculation, a Ceff/Cmin concentration of 10-15 nM is used[1].
[1]. Mowbray CE, et al. Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6596-602.
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