| Bioactivity | Adriforant hydrochloride (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. |
| Target | Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func) |
| Invitro | 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 nM is used[1]. |
| Name | Adriforant hydrochloride |
| CAS | 2096455-90-0 |
| Formula | C13H25Cl3N6 |
| Molar Mass | 371.74 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |
Adriforant hydrochloride
CAS: 2096455-90-0 F: C13H25Cl3N6 W: 371.74
Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4
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