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Adriforant hydrochloride

CAS No. : 2096455-90-0

MCE 站：Adriforant hydrochloride

产品活性：Adriforant hydrochloride (PF-3893787 hydrochloride) 是一种新型组胺 H4 受体亲和型拮抗剂 (K_i=2.4 nM)，也是一种H4 受体功能性拮抗剂 (K_i=1.56 nM)。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: Adriforant is tested and observed binding K_i=2.4 nM and functional K_i=1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and Adriforant (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.

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