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.