1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. VUF10460

VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

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

VUF10460 Chemical Structure

VUF10460 Chemical Structure

CAS No. : 1028327-66-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 385 In-stock
100 mg USD 605 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.

IC50 & Target

H4 receptor

 

In Vitro

UF10460 binds to rat H3 and H4 receptor with pKi values of 5.75, and 7.46, respectively. VUF10460 displays approximately a 50-fold selectivity for the rat H4 receptor over the H3 receptor[1].

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

In Vivo

HCl-induced rat gastric lesions is significantly enhanced by the H4 receptor agonists VUF10460. This effect is not modified by H4 receptor antagonist JNJ7777120[1].

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

Molecular Weight

269.34

Formula

C15H19N5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=NC(C2=CC=CC=C2)=CC(N3CCN(C)CC3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (371.28 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 3.7128 mL 18.5639 mL 37.1278 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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:

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 (9.28 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 (9.28 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).
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]

Rats: VUF10460 is dissolved in 100% DMSO. Gastric lesions are induced in 24 h fasted rats by a single intragastric administration of 0.6 N HCl (5mL/kg volume). Drugs under study are administered subcutaneously 30 min before HCl. Rats are randomly divided to receive single doses (10 and/or 30 mg/kg) of immethridine, methimepip, immepip, VUF8430, VUF10460 or the vehicle, in a 1 mL/kg volume[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7128 mL 18.5639 mL 37.1278 mL 92.8195 mL
5 mM 0.7426 mL 3.7128 mL 7.4256 mL 18.5639 mL
10 mM 0.3713 mL 1.8564 mL 3.7128 mL 9.2819 mL
15 mM 0.2475 mL 1.2376 mL 2.4752 mL 6.1880 mL
20 mM 0.1856 mL 0.9282 mL 1.8564 mL 4.6410 mL
25 mM 0.1485 mL 0.7426 mL 1.4851 mL 3.7128 mL
30 mM 0.1238 mL 0.6188 mL 1.2376 mL 3.0940 mL
40 mM 0.0928 mL 0.4641 mL 0.9282 mL 2.3205 mL
50 mM 0.0743 mL 0.3713 mL 0.7426 mL 1.8564 mL
60 mM 0.0619 mL 0.3094 mL 0.6188 mL 1.5470 mL
80 mM 0.0464 mL 0.2320 mL 0.4641 mL 1.1602 mL
100 mM 0.0371 mL 0.1856 mL 0.3713 mL 0.9282 mL
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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.

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Product Name:
VUF10460
Cat. No.:
HY-101420
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