2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. GSK2239633A

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96?±?0.11.

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GSK2239633A Chemical Structure

GSK2239633A Chemical Structure

CAS No. : 1240516-71-5

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Based on 1 publication(s) in Google Scholar

GSK2239633A Related Antibodies

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96?±?0.11.

IC50 & Target[1]

[125I]-TARC-CCR4

7.96 (pIC50)

In Vitro

The GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with a pA2 of 7.11±0.29[1]. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4+ CCR4+ T cells is measured. The pEC50 value is 8.79±0.22[2].

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

GSK2239633A Related Antibodies
In Vivo

Following intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t1/2: 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach Cmax rapidly (median tmax: 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%[1]. GSK2239633A (Compound 9) demonstrates good pharmacokinetic data in preclinical animal studies (bioavailability in rats and beagle dogs 85% and 97% respectively)[3].

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

549.06

Formula

C24H25ClN4O5S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(O)C(NCC1=CC=CC(CN2N=C(NS(=O)(C3=CC=C(Cl)S3)=O)C4=C2C=CC=C4OC)=C1)=O
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 (455.32 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 1.8213 mL 9.1065 mL 18.2129 mL
5 mM 0.3643 mL 1.8213 mL 3.6426 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
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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 (3.79 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.79 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

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

Purity: 99.81%

COA (261 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

Blood is taken from normal volunteers who have taken no medication within the previous 10 days and chemokine-induced increases in the filamentous (F)-actin content of CD4+ CCR4+ T cells are measured. Briefly, the peripheral blood mononuclear cells (PBMC) are isolated and stained with fluorescein isothiocyanate-conjugated anti-human CD4 and phycoerythrin-conjugated anti-CCR4 antibodies. The cells are then incubated with GSK2239633A (1 μM) or vehicle (0.1% DMSO) for 30 min at 37°C before stimulation with agonist for 15 sec. The assay is terminated by addition of 3% formaldehyde. The fixed cells are stained with Alexa fluor-647 phalloidin and the mean fluorescence intensity of 1000 CD4+ CCR4+ cells per sample is determined. This is expressed as a fraction of the mean intensity of the CD4+ CCR4- cells in the same sample[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Rats and Dogs[3]
Pharmacokinetics are determined in male Wistar Han rats (277-305 g) or male Sprague Dawley (crl:CD(SD)) rats 277-305 g) and male Beagle dogs (14-16 kg; aged approximately 3-4 years) following single oral and intravenous administration to aid prediction of the likely human pharmacokinetics using precedented physiological scaling techniques. In the rat, compounds (e.g., GSK2239633A) are dosed intravenously and orally to 2 rats per compound per route. Nominal doses of 1 mg/kg are used for intravenous (iv) and oral (po) administration and studies are conducted following routine animal husbandry methods. Rats are housed in standard holding cages and maintained in a controlled environment with free access to food and water. Serial blood samples are collected via a temporary cannula inserted into the tail vein of all animals. For the intravenously dosed animals the cannula is inserted into a vein discrete from that used for dosing. The dogs are kept in slings for no longer than 2 h following the end of dosing on each phase of the study. Compounds (e.g., GSK2239633A) are dosed intravenously (bolus, 0.5 mg/kg) using an angiocath and orally (gavage; 1 mg/kg) to two male Beagle dogs per compound in a cross over design. Serial blood samples are collected from the cephalic vein via an angiocath for the first 2 h post dose and via direct venipuncture for the remainder of the study.

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 1.8213 mL 9.1065 mL 18.2129 mL 45.5324 mL
5 mM 0.3643 mL 1.8213 mL 3.6426 mL 9.1065 mL
10 mM 0.1821 mL 0.9106 mL 1.8213 mL 4.5532 mL
15 mM 0.1214 mL 0.6071 mL 1.2142 mL 3.0355 mL
20 mM 0.0911 mL 0.4553 mL 0.9106 mL 2.2766 mL
25 mM 0.0729 mL 0.3643 mL 0.7285 mL 1.8213 mL
30 mM 0.0607 mL 0.3035 mL 0.6071 mL 1.5177 mL
40 mM 0.0455 mL 0.2277 mL 0.4553 mL 1.1383 mL
50 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.9106 mL
60 mM 0.0304 mL 0.1518 mL 0.3035 mL 0.7589 mL
80 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
100 mM 0.0182 mL 0.0911 mL 0.1821 mL 0.4553 mL
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GSK2239633A Related Classifications

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  • 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:

GSK2239633A1240516-71-5CCRCC chemokine receptorInhibitorinhibitorinhibit

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