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PF-3893787 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PF-3893787 hydrochloride图片
CAS NO:2096455-90-0
规格:98%
分子量:371.74
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
PF-3893787hydrochloride是一种新型组胺H4受体亲和型拮抗剂(Ki=2.4nM),也是一种H4受体功能性拮抗剂(Ki=1.56nM)。
CAS:2096455-90-0
分子式:C13H25Cl3N6
分子量:371.74
纯度:98%
存储:Store at -20°C

Background:

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.