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

Adriforant hydrochloride  (Synonyms: PF-3893787 hydrochloride)

Cat. No.: HY-19705B Purity: ≥98.0%
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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

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Based on 1 publication(s) in Google Scholar

Other Forms of Adriforant hydrochloride:

Adriforant hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Adriforant hydrochloride

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Adriforant hydrochloride Related Antibodies
Clinical Trial
Molecular Weight

371.74

Formula

C13H25Cl3N6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC(N2C[C@H](NC)CC2)=CC(NCC3CC3)=N1.[H]Cl.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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.

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
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (269.01 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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.

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Adriforant hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Adriforant2096455-90-0PF-3893787PF3893787PF 3893787Histamine ReceptorInhibitorinhibitorinhibit

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