Adriforant hydrochloride
Based on 2 publication(s) in Google Scholar
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.
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- Reinheit : 98.0%
- CAS. Nr.: 2096455-90-0
- Formel: C13H25Cl3N6
- Molecular Weight:371.74
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Adriforant hydrochloride
MoreAlle Histamine Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2096455-90-0
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Appearance Solid
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Molecular Weight 371.74
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Formel C13H25Cl3N6
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Color White to off-white
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SMILES
NC1=NC(N2C[C@H](NC)CC2)=CC(NCC3CC3)=N1.[H]Cl.[H]Cl.[H]Cl
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Synonyms
PF-3893787 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Decoding ligand recognition and constitutive activation of histamine H3 and H4 receptors. [Abstract]2025 Aug 28. PMID: 40877594 -
Behav Brain Res
Differential roles of prelimbic and anterior cingulate cortical region in the modulation of histaminergic and non-histaminergic itch. [Abstract]2021 Aug 6:411:113388. PMID: 34052263
Lösungsmittel & Löslichkeit
In Vitro:
H2O : 100 mg/mL (269.01 mM; Need ultrasonic)
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.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (269.01 mM); Clear solution; Need ultrasonic
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.6901 mL | 13.4503 mL | 26.9005 mL | 67.2513 mL |
| 5 mM | 0.5380 mL | 2.6901 mL | 5.3801 mL | 13.4503 mL | |
| 10 mM | 0.2690 mL | 1.3450 mL | 2.6901 mL | 6.7251 mL | |
| 15 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL | 4.4834 mL | |
| 20 mM | 0.1345 mL | 0.6725 mL | 1.3450 mL | 3.3626 mL | |
| 25 mM | 0.1076 mL | 0.5380 mL | 1.0760 mL | 2.6901 mL | |
| 30 mM | 0.0897 mL | 0.4483 mL | 0.8967 mL | 2.2417 mL | |
| 40 mM | 0.0673 mL | 0.3363 mL | 0.6725 mL | 1.6813 mL | |
| 50 mM | 0.0538 mL | 0.2690 mL | 0.5380 mL | 1.3450 mL | |
| 60 mM | 0.0448 mL | 0.2242 mL | 0.4483 mL | 1.1209 mL | |
| 80 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8406 mL | |
| 100 mM | 0.0269 mL | 0.1345 mL | 0.2690 mL | 0.6725 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Adriforant hydrochloride Related Classifications
HY-19705B Related Classifications
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