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)。

Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (K i =2.4 nM) and is also a functional (K i =1.56 nM) antagonist.

Solid

Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)

Adriforant 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 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

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: H₂O : 100 mg/mL (269.01 mM; Need ultrasonic)DMSO : ≥ 83.33 mg/mL (224.16 mM)