Adriforant hydrochloride - 10mM in DMSO , CAS No.2096455-90-0

CAS: 2096455-90-0 Cat. No.: A656356 Molecular Weight: 371.74 PubChem CID: 131801117

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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.

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 IC 50 on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Desiccated, Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Names and Identifiers

• PubChem CID: 131801117
• Molecular Weight: 371.74