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Submit ReviewGSK 2239633A
Description: Potent CCR4 antagonist
Chemical Name: N-[[3-[[3-[[(5-Chloro-2-thienyl)sulfonyl]amino]-4-methoxy-1H-indazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide
Purity: ≥98% (HPLC)
Biological Activity for GSK 2239633A
GSK 2239633A is a potent CCR4 antagonist (pIC50 = 7.83 in a 35S-GTPγS competition assay). Inhibits thymus activation-regulated chemokine (TARC) -induced F-actin polymerization in human whole blood.
Technical Data for GSK 2239633A
| M. Wt | 549.06 |
| Formula | C24H25ClN4O5S2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1240516-71-5 |
| PubChem ID | 46861584 |
| InChI Key | YTEVTHHGQMUPHC-UHFFFAOYSA-N |
| Smiles | COC1=C2C(NS(=O)(C3=CC=C(S3)Cl)=O)=NN(C2=CC=C1)CC4=CC(CNC(C(C)(O)C)=O)=CC=C4 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK 2239633A
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 54.91 | 100 |
Preparing Stock Solutions for GSK 2239633A
The following data is based on the product molecular weight 549.06. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.82 mL | 9.11 mL | 18.21 mL |
| 5 mM | 0.36 mL | 1.82 mL | 3.64 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.82 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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Product Datasheets for GSK 2239633A
References for GSK 2239633A
References are publications that support the biological activity of the product.
Procopiou et al (2012) Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation. Bioorg.Med.Chem.Lett. 22 2730 PMID: 22437117
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Keywords: GSK 2239633A, GSK 2239633A supplier, GSK2239633A, CCR4, antagonists, antagonism, potent, TARC, CCL17, thymus, activation-regulated, chemokines, CCL22, macrophage-derived, MDC, Chemokine, CC, Receptors, 7071, Tocris Bioscience
Citations for GSK 2239633A
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