1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. Adriforant hydrochloride

Adriforant hydrochloride (Synonyms: PF-3893787 (hydrochloride))

Cat. No.: HY-19705B Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Adriforant hydrochloride Chemical Structure

Adriforant hydrochloride Chemical Structure

CAS No. : 2096455-90-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 311 In-stock
Estimated Time of Arrival: December 31
1 mg USD 130 In-stock
Estimated Time of Arrival: December 31
5 mg USD 380 In-stock
Estimated Time of Arrival: December 31
10 mg USD 630 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1260 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2770 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Description

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.

IC50 & Target

Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)[1]

In Vitro

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].

Molecular Weight

371.74

Formula

C₁₃H₂₅Cl₃N₆

CAS No.

2096455-90-0

SMILES

NC1=NC(N2C[[email protected]](NC)CC2)=CC(NCC3CC3)=N1.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.33 mg/mL (224.16 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6901 mL 13.4503 mL 26.9005 mL
5 mM 0.5380 mL 2.6901 mL 5.3801 mL
10 mM 0.2690 mL 1.3450 mL 2.6901 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
Adriforant hydrochloride
Cat. No.:
HY-19705B
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