Referencia número: HY-123205

Oxatomide

(Synonyms: KW-4354)

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Based on 1 Customer Validation

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.

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Pureza: 98.11%
No. CAS: 60607-34-3
Fòrmula: C₂₇H₃₀N₄O
Peso molecular:426.55

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Oxatomide Chemical Structure

No. CAS: 60607-34-3

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

P2X7 Receptor

H₁ Receptor

serotonin

COX-2

Ver todos los productos específicos de isoformas Histamine Receptor :

Ver todos los productos específicos de isoformas P2X Receptor :

Ver todos los productos específicos de isoformas 5-HT Receptor :

Ver todos los productos específicos de isoformas p38 MAPK :

Ver todos los productos específicos de isoformas COX :

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	EC₅₀	0.4 μM Compound: Oxatomide	Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4 Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4	[PMID: 20966043]
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.

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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 60607-34-3
Appearance Solid
Peso molecular 426.55
Fòrmula C₂₇H₃₀N₄O
Color White to off-white
SMILES

O=C1NC2=CC=CC=C2N1CCCN3CCN(C(C4=CC=CC=C4)C5=CC=CC=C5)CC3
Synonyms

KW-4354
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3444 mL

11.7220 mL

23.4439 mL

5 mM

0.4689 mL

2.3444 mL

4.6888 mL

10 mM

0.2344 mL

1.1722 mL

2.3444 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Kazuki Yoshida, et al. P2X7 receptor antagonist activity of the anti-allergic agent oxatomide. Eur J Pharmacol. 2015 Nov 15;767:41-51. [Content Brief]

[2]. Domae M, et al. The antiallergic drug oxatomide promotes human eosinophil apoptosis and suppresses IL-5-induced eosinophil survival. J Allergy Clin Immunol. 2003 Mar;111(3):567-72. [Content Brief]

[3]. Patella V, et al. Oxatomide inhibits the release of proinflammatory mediators from human basophils and mast cells. Int Arch Allergy Immunol. 1996 Sep;111(1):23-9. [Content Brief]

[4]. Tanaka T,et al. Effect of oxatomide on otitis media with effusion--an experimental study. Acta Otolaryngol. 1995 Jul;115(4):532-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Ver todos los productos específicos de isoformas Histamine Receptor

Ver todos los productos específicos de isoformas P2X Receptor

Ver todos los productos específicos de isoformas 5-HT Receptor

Ver todos los productos específicos de isoformas p38 MAPK

Ver todos los productos específicos de isoformas COX

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Oxatomide Related Classifications

HY-123205 Related Classifications