2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. JNJ10191584

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.

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JNJ10191584 Chemical Structure

JNJ10191584 Chemical Structure

CAS No. : 73903-17-0

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25 mg USD 307 In-stock
50 mg USD 507 In-stock
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Based on 1 publication(s) in Google Scholar

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JNJ10191584 Related Antibodies

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Description

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].

IC50 & Target

Human H4 Receptor

26 nM (Ki)

human H3 receptor

14.1 μM (Ki)

In Vitro

JNJ10191584 shows binding affinity of 26 nM and 14.1 μM to H4 and H3 receptor, respectively[1].
JNJ10191584 (3 h) shows inhibitory effects to chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1].

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

JNJ10191584 Related Antibodies
In Vivo

JNJ10191584 (10 μg/μL; intra locus coeruleus (LC) administration; once) abolishs VUF-induced anti-allodynic effect in spared nerve injury (SNI) mice[1].
JNJ10191584 (10 μg/μL; intra LC administration; once) prevents the anti-allodynic effect of VUF 8430 in SNI mice[1].
JNJ10191584 (6 μg/mouse; intrathecal administration; pretreat once) prevents VUF 8430-induced anti-allodynic effect in SNI mice[1].

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

278.74

Formula

C13H15ClN4O
CAS No.
SMILES

O=C(N1CCN(CC1)C)C2=NC3=CC(Cl)=CC=C3N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (179.38 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 3.5876 mL 17.9379 mL 35.8757 mL
5 mM 0.7175 mL 3.5876 mL 7.1751 mL
View the Complete Stock Solution Preparation Table

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  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (17.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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).
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

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5876 mL 17.9379 mL 35.8757 mL 89.6893 mL
5 mM 0.7175 mL 3.5876 mL 7.1751 mL 17.9379 mL
10 mM 0.3588 mL 1.7938 mL 3.5876 mL 8.9689 mL
15 mM 0.2392 mL 1.1959 mL 2.3917 mL 5.9793 mL
20 mM 0.1794 mL 0.8969 mL 1.7938 mL 4.4845 mL
25 mM 0.1435 mL 0.7175 mL 1.4350 mL 3.5876 mL
30 mM 0.1196 mL 0.5979 mL 1.1959 mL 2.9896 mL
40 mM 0.0897 mL 0.4484 mL 0.8969 mL 2.2422 mL
50 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7938 mL
60 mM 0.0598 mL 0.2990 mL 0.5979 mL 1.4948 mL
80 mM 0.0448 mL 0.2242 mL 0.4484 mL 1.1211 mL
100 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
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JNJ10191584 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:

JNJ1019158473903-17-0VUF6002JNJ 10191584JNJ-10191584VUF 6002VUF-6002Histamine Receptorbenzimidazolechemotaxiseosinophilsmast cellsselectiveoralanti-allodyniclocus coeruleusVUF 8430Inhibitorinhibitorinhibit

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