CRTh2 antagonist 3
CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2].
Product Specifications
CAS Number
312928-72-6
UNSPSC
12352005
Target
PDK-1; Prostaglandin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; PI3K/Akt/mTOR
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/crth2-antagonist-3.html
Solubility
10 mM in DMSO
Smiles
O=C(O)CN1C2=CC=CC=C2N=C1SCCOC3=C(C)C=CC=C3C
Molecular Formula
C19H20N2O3S
Molecular Weight
356.44
References & Citations
[1]Heinz Fretz, et al. 2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists. US8273740B2.|[2]Rettenmaier TJ, et al. Small-Molecule Allosteric Modulators of the Protein Kinase PDK1 from Structure-Based Docking. J Med Chem. 2015 Oct 22;58 (20) :8285-8291.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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