Adriforant

SKU: orb1741200

Description

Adriforant is a potent and selective competitive antagonist of the histamine H4 receptor. It inhibits histamine-driven ERK phosphorylation, calcium mobilization, and gene expression changes, demonstrating efficacy in reducing itch and inflammatory responses in murine models of skin inflammation.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 943057-12-3
• MW: 262.35
• Purity: 99.84% (May vary between batches)
• Formula: C₁₃H₂₂N₆
• SMILES: N(C)[C@H]1CN(CC1)C=2C=C(NCC3CC3)N=C(N)N2
• Target: Histamine Receptor

Bioactivity

• Target IC50:
  Actin polymerization (eosinophils):1.3 nM|CD11b expression (eosinophils):4.9 nM|Eosinophil cell shape change:0.65 nM
• In Vivo:
  Adriforant was administered orally (5 mg/kg, p.o.) and intravenously (1 mg/kg, i.v.) in rats, showing good pharmacokinetics (T₁/₂ = 7 h, F = 62%). In dogs, oral dosing (10 mg/kg, p.o.) also showed favorable exposure (T₁/₂ = 24 h, F = 39%). In 7-day repeat-dose toxicity studies in rats and monkeys, no adverse effects were observed at free plasma concentrations up to 187–240× the predicted minimum human efficacious level.
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• In Vitro:
  Adriforant was tested in various human eosinophil functional assays, including cell shape change (IC₅₀ = 0.65 nM), CD11b expression (IC₅₀ = 4.9 nM), and actin polymerization (IC₅₀ = 1.3 nM). In a whole blood granulocyte assay (GAFS), Adriforant fully blocked imetit-induced responses at 30 nM. The binding affinity (Ki) for human H4R was 2.4 nM, with a functional Ki of 1.56 nM, indicating potent and selective H4R antagonism.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Adriforant, PF03893787, PF-03893787, PF 3893787, PF3893787, PF-3893787, PF 03893787, ZPL 389, ZPL 3893787, ZPL389, ZPL-389, ZPL3893787, ZPL3893797, ZPL-3893797

Compound Identifiers

PubChem CID

24745335