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Adriforant
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Catalog No. T68280Cas No. 943057-12-3
Alias ZPL-3893797, ZPL3893797, ZPL-389, ZPL389, PF-3893787, PF3893787
Adriforant (PF-3893787,ZPL-3893797) is a competitive H4 (histamine receptor 4) antagonist that antagonizes histamine-induced phosphorylation of ERK, normalizes histamine-induced transcriptional changes in mast cells and reduces histamine-dependent Ca2+ fluxes in neurons, which alleviates itching and skin inflammation in mice
Adriforant
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Purity: 99.84%
Catalog No. T68280Alias ZPL-3893797, ZPL3893797, ZPL-389, ZPL389, PF-3893787, PF3893787Cas No. 943057-12-3
Adriforant (PF-3893787,ZPL-3893797) is a competitive H4 (histamine receptor 4) antagonist that antagonizes histamine-induced phosphorylation of ERK, normalizes histamine-induced transcriptional changes in mast cells and reduces histamine-dependent Ca2+ fluxes in neurons, which alleviates itching and skin inflammation in mice
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $293 | - | In Stock | |
| 5 mg | $722 | - | In Stock | |
| 10 mg | $987 | - | In Stock | |
| 25 mg | $1,520 | - | In Stock | |
| 50 mg | $1,980 | - | In Stock | |
| 100 mg | $2,500 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.84%
Appearance:Viscous
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Adriforant (PF-3893787,ZPL-3893797) is a competitive H4 (histamine receptor 4) antagonist that antagonizes histamine-induced phosphorylation of ERK, normalizes histamine-induced transcriptional changes in mast cells and reduces histamine-dependent Ca2+ fluxes in neurons, which alleviates itching and skin inflammation in mice |
| Targets&IC50 | Eosinophil cell shape change:0.65 nM, Actin polymerization (eosinophils):1.3 nM, CD11b expression (eosinophils):4.9 nM |
| 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[1]. |
| 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[1]. |
| Synonyms | ZPL-3893797, ZPL3893797, ZPL-389, ZPL389, PF-3893787, PF3893787 |
| Molecular Weight | 262.35 |
| Formula | C13H22N6 |
| Cas No. | 943057-12-3 |
| Smiles | N(C)[C@H]1CN(CC1)C=2C=C(NCC3CC3)N=C(N)N2 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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