GSK 2239633A - ≥98%(HPLC), high purity , CAS No.1240516-71-5, Antagonist of CCR4;Antagonist of CCR5

Item Number
G286917
Grouped product items
SKUSizeAvailabilityPrice Qty
G286917-1mg
1mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$37.90
G286917-5mg
5mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$154.90
G286917-10mg
10mg
2
$199.90
G286917-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$578.90
G286917-50mg
50mg
1
$699.90

Potent CCR4 antagonist

Basic Description

SynonymsPropanamide, N-((3-((3-(((5-chloro-2-thienyl)sulfonyl)amino)-4-methoxy-1H-indazol-1-yl)methyl)phenyl)methyl)-2-hydroxy-2-methyl- | GTPL10416 | A929738 | BCP29621 | UNII-07ODS257BP | MS-30054 | SCHEMBL358731 | AKOS040733312 | N-((3-((3-((5-Chloro-2-thienyl
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent CCR4 antagonist (pIC50= 7.83 in a35S-GTPγS competition assay). Inhibits thymus activation-regulated chemokine (TARC) -induced F-actin polymerization in human whole blood.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of CCR4;Antagonist of CCR5
Product 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.

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Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid504770823
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/504770823
IUPAC Name N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide
INCHI InChI=1S/C24H25ClN4O5S2/c1-24(2,31)23(30)26-13-15-6-4-7-16(12-15)14-29-17-8-5-9-18(34-3)21(17)22(27-29)28-36(32,33)20-11-10-19(25)35-20/h4-12,31H,13-14H2,1-3H3,(H,26,30)(H,27,28)
InChi Key YTEVTHHGQMUPHC-UHFFFAOYSA-N
Canonical SMILES CC(C)(C(=O)NCC1=CC(=CC=C1)CN2C3=C(C(=CC=C3)OC)C(=N2)NS(=O)(=O)C4=CC=C(S4)Cl)O
Isomeric SMILES CC(C)(C(=O)NCC1=CC(=CC=C1)CN2C3=C(C(=CC=C3)OC)C(=N2)NS(=O)(=O)C4=CC=C(S4)Cl)O
PubChem CID 46861584
Molecular Weight 549.06

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

7 results found

Lot NumberCertificate TypeDateItem
K2316172Certificate of AnalysisNov 07, 2023 G286917
K2316173Certificate of AnalysisNov 07, 2023 G286917
K2316336Certificate of AnalysisNov 07, 2023 G286917
K2316337Certificate of AnalysisNov 07, 2023 G286917
K2316338Certificate of AnalysisNov 07, 2023 G286917
K2316339Certificate of AnalysisNov 07, 2023 G286917
K2316340Certificate of AnalysisNov 07, 2023 G286917

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References

1. Procopiou PA, Barrett JW, Barton NP, Begg M, Clapham D, Copley RC, Ford AJ, Graves RH, Hall DA, Hancock AP et al..  (2013)  Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists..  J Med Chem,  56  (5): (1946-60).  [PMID:23409871] [10.1021/op500134e]
2. Cahn A, Hodgson S, Wilson R, Robertson J, Watson J, Beerahee M, Hughes SC, Young G, Graves R, Hall D et al..  (2013)  Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study..  BMC Pharmacol Toxicol,  14  (13): (14).  [PMID:23448278] [10.1186/2050-6511-14-14]

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