2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Membrane Transporter/Ion Channel Apoptosis Cell Cycle/DNA Damage MAPK/ERK Pathway
  3. Histamine Receptor P2X Receptor 5-HT Receptor Apoptosis PERK p38 MAPK COX
  4. Oxatomide

Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.

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

Oxatomide Chemical Structure

Oxatomide Chemical Structure

CAS No. : 60607-34-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Oxatomide:

Oxatomide Related Antibodies

Top Publications Citing Use of Products

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

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5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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COX COX-1 COX-2 COX-3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases[1][2][3][4].

IC50 & Target[1]

P2X7 Receptor

 

H1 Receptor

 

serotonin

 

COX-2

 

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
25.1 μM
Compound: Oxatomide
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
HepG2 EC50
3.5 μM
Compound: Oxatomide
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
[PMID: 20966043]
HepG2 EC50
7.1 μM
Compound: Oxatomide
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
[PMID: 20966043]
In Vitro

Oxatomide (1-30 μM; 0-60 s) inhibits the elevation of [Ca2+]i induced by 1 mM ATP in N18TG2 cells, with an IC50 of 3.37 μM[1].
Oxatomide (10 μM; pre-treatment) inhibits the phosphorylation of ERK and p38 MAPK induced by ATP in N18TG2 cells[1].
Oxatomide (10 μM; pre-treatment) inhibits the upregulation of COX-2 and MIP-2 mRNA and the secretion of MIP-2 induced by BzATP in J774 macrophages[1].
Oxatomide (0-30 μM; 0-48 h) can promote the apoptosis of peripheral blood eosinophils and inhibit the survival induced by IL-5[2].
Oxatomide (0.1-10 μM; 15 min) inhibits the immunological release of histamine and LTC4 in human basophils[3].
Oxatomide (0.1-10 μM; 15 min) inhibits the release of histamine, tryptase and PGD2 after stimulation by anti-IgE or anti-FcεRI in human skin mast cells[3].

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

Oxatomide Related Antibodies
In Vivo

Oxatomide (5-30 mg/kg; oral gavage; 5 days-2 weeks) has a beneficial effect in the chinchilla model of immune-mediated exudative otitis media[4].

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

Animal Model: Healthy chinchillas (350-600 g) with immune-mediated otitis media model[4]
Dosage: 5, 10 and 30 mg/kg
Administration: Oral gavage; 5 days and 2 weeks
Result: Alleviated the experimental otitis media with effusion at doses of 10 and 30 mg/kg.
Significantly reduced the mean LTD4 concentration in middle ear effusion at dose of 30 mg/kg.
Was rapidly absorbed and transported to the middle ear by oral administration.
Clinical Trial
Molecular Weight

426.55

Formula

C27H30N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC=CC=C2N1CCCN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
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 : 250 mg/mL (586.10 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 2.3444 mL 11.7220 mL 23.4439 mL
5 mM 0.4689 mL 2.3444 mL 4.6888 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: ≥ 2.08 mg/mL (4.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

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 2.3444 mL 11.7220 mL 23.4439 mL 58.6098 mL
5 mM 0.4689 mL 2.3444 mL 4.6888 mL 11.7220 mL
10 mM 0.2344 mL 1.1722 mL 2.3444 mL 5.8610 mL
15 mM 0.1563 mL 0.7815 mL 1.5629 mL 3.9073 mL
20 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9305 mL
25 mM 0.0938 mL 0.4689 mL 0.9378 mL 2.3444 mL
30 mM 0.0781 mL 0.3907 mL 0.7815 mL 1.9537 mL
40 mM 0.0586 mL 0.2930 mL 0.5861 mL 1.4652 mL
50 mM 0.0469 mL 0.2344 mL 0.4689 mL 1.1722 mL
60 mM 0.0391 mL 0.1954 mL 0.3907 mL 0.9768 mL
80 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7326 mL
100 mM 0.0234 mL 0.1172 mL 0.2344 mL 0.5861 mL
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Oxatomide 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:

Oxatomide60607-34-3KW-4354KW4354KW 4354Histamine ReceptorP2X Receptor5-HT ReceptorApoptosisPERKp38 MAPKCOXP2XRsSerotonin Receptor5-hydroxytryptamine ReceptorProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseCyclooxygenaseP2X7anti-allergicantihistamineATPCa2+serotoninH1-histamineimmune-mediated otitis media modelN18TG2 cellsJ774 macrophagesperipheral blood eosinophilshuman basophilshuman skin mast cellsInhibitorinhibitorinhibit

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