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

Toreforant  (Synonyms: JNJ-38518168)

Cat. No.: HY-16756 Purity: 99.82%
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Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.

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

Toreforant Chemical Structure

Toreforant Chemical Structure

CAS No. : 952494-46-1

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Based on 1 publication(s) in Google Scholar

Toreforant Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.

IC50 & Target

H4 receptor

8.4±2.2 nM (IC50)

In Vitro

In human polymorphonuclear leukocytes, Toreforant inhibits the histamine-induced shape change of human eosinophils and produces a rightward shift in the histamine dose response curves indicating that it is acting as an antagonist of the human H4R in these primary cells. This is not an equilibrium measurement and therefore the calculation of a pA2 is complicated. The pA2 can be estimated using the shift seen the lowest concentration of antagonist. This yields a pA2 of around 7.5 consistent with the results in the transfected system. This assay can also be performed in whole blood and, as for the purified cells, Toreforant is able to inhibit the actions of histamine. The IC50 values are 296 nM and 780 nM when 100 nM and 300 nM histamine are used, respectively[1].

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

Toreforant Related Antibodies
In Vivo

The animals treated with 100 mg/kg toreforant have reduced disease severity scores. The reduction in scores is similar to JNJ 28307474. A model of histamine-induced scratching in CD-1 mice (n=5 per group) is used to judge the anti-pruritic effects of Toreforant. Unlike other H4R antagonists, Toreforant is not efficacious in reducing histamine-mediated pruritus. After oral administration to rats, Toreforant-derived radioactivity is widely distributed into tissues; however, it is not quantifiable in cerebellum, cerebrum, medulla, and spinal cord in either Long Evans or Sprague Dawley rats, suggesting that drug-derived radioactivity does not cross the blood-brain barrier. Neuropathic pain models in rats are conducted with Toreforant and an H4R antagonist that does cross the blood-brain barrier, JNJ 39758979. In a rat spinal nerve ligation model JNJ 39758979 was able to significantly attenuate the mechanical allodynia induced in the model, however Toreforant has no activity[1].

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

392.54

Formula

C23H32N6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1CCC(CCCNC2=NC=C(C3=NC4=CC(C)=CC(C)=C4N3)C(C)=N2)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (254.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5475 mL 12.7376 mL 25.4751 mL
5 mM 0.5095 mL 2.5475 mL 5.0950 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • 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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Animal Administration
[1]

Mice[1]
The ovalbumin mouse asthma model and the collageninduced arthritis model are conducted. Toreforant is dosed orally in 20% hydroxypropyl-β-cyclodextrin. In the collagen-induced arthritis model Toreforant is given orally twice a day starting with the first signs of disease onset around Day 30 and continued for 14 days. CD-1 mice (5 per group) are dosed with vehicle (20% hydroxypropyl-β-cyclodextrin), Toreforant or JNJ 28307474, as a positive control, at 50 mg/kg orally, 60 mins prior to the intra-dermal injection of histamine. Bouts of scratching are recorded over a 20 minute period. In a subsequent experiment mice are orally dosed with Toreforant (100 mg/kg) at 24, 8, 4 and 1 h prior to intra-dermal injection of histamine and similarly monitored. The area at the back of the neck of mice is shaved 24 hours prior to an intra-dermal injection of 20 μL of 100 μg compound 48/80. Both knockout and wild-type mice (five mice per group) are dosed with vehicle, Toreforant (50 mg/kg) or JNJ 28307474 (50 mg/kg), orally, 60 mins prior to the intradermal injection. Bouts of scratching are recorded over a 20 minute period. Terminal (t=80 min) plasma and brain samples are analyzed for drug concentration. Male Sprague-Dawley rats are deeply anesthetized with isoflurane/oxygen inhalational anesthesia [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 and light). 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 1 mM 2.5475 mL 12.7376 mL 25.4751 mL 63.6878 mL
5 mM 0.5095 mL 2.5475 mL 5.0950 mL 12.7376 mL
10 mM 0.2548 mL 1.2738 mL 2.5475 mL 6.3688 mL
15 mM 0.1698 mL 0.8492 mL 1.6983 mL 4.2459 mL
20 mM 0.1274 mL 0.6369 mL 1.2738 mL 3.1844 mL
25 mM 0.1019 mL 0.5095 mL 1.0190 mL 2.5475 mL
30 mM 0.0849 mL 0.4246 mL 0.8492 mL 2.1229 mL
40 mM 0.0637 mL 0.3184 mL 0.6369 mL 1.5922 mL
50 mM 0.0510 mL 0.2548 mL 0.5095 mL 1.2738 mL
60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0615 mL
80 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7961 mL
100 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6369 mL
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Toreforant 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:

Toreforant952494-46-1JNJ-38518168JNJ38518168JNJ 38518168Histamine ReceptorInhibitorinhibitorinhibit

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