| Field | Specification |
|---|---|
| Alternative names | PF-3893787 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C13H25Cl3N6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel antagonist of the histamine H4 receptor, with a binding affinity Ki of 2.4 nM and a functional Ki of 1.56 nM. It is supplied as a white to off-white solid (C13H25Cl3N6, MW 371.74) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 2096455-90-0 |
|---|---|
| Molecular Formula | C13H25Cl3N6 |
| Molecular Weight | 371.74 g/mol |
| Purity | 98.0% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | NC1=NC(N2C[C@H](NC)CC2)=CC(NCC3CC3)=N1.[H]Cl.[H]Cl.[H]Cl |
| Signaling Pathway | GPCR/G Protein; Neuronal Signaling; Immunology/Inflammation |
| Solubility | In Vitro: H2O: 100 mg/mL (269.01 mM; Requires sonication) DMSO: ≥ 83.33 mg/mL (224.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
Activity & Target
Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 100 mg/mL (269.01 mM) | requires sonication |
| DMSO | ≥ 83.33 mg/mL (224.16 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration. Percentages are volume ratios of the final working solution. Prepare the working solution fresh on the day of dosing; if precipitation or phase separation occurs, gentle warming or sonication can help.
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 1
| Composition | PBS |
|---|---|
| Result | 100 mg/mL (269.01 mM); clear solution; requires sonication |
Data provided by the manufacturer.
In Vitro
For H4R, Adriforant is observed to bind with Ki=2.4 nM and to have a functional Ki=1.56 nM in testing. Projections of the free plasma efficacious concentration converge across functional assays, and on rhH4R, Adriforant is fast on/fast off. With human native isolated eosinophils, the in vitro IC50 measured by actin polymerisation is 1.16 nM; assuming 10 times the IC50 is needed for >90% receptor occupancy (and so close to complete inhibition of the response), a concentration of 12 nM was suggested. In the whole blood GAFS assay, a total blood concentration of 30 nM completely blocks the imetit induced shape change (approximately 10 nM free once PPB and blood partitioning are corrected for). A Ceff/Cmin concentration of 10-15 nM is used for dose projection and safety margin calculation[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Decoding ligand recognition and constitutive activation of histamine H3 and H4 receptors. Acta Pharmacol Sin 2025 Aug 28. PMID: 40877594
Differential roles of prelimbic and anterior cingulate cortical region in the modulation of histaminergic and non-histaminergic itch. Behav Brain Res 2021 Aug 6:411:113388. PMID: 34052263
