Teijin compound 1
Names
Biological Activity
[Description]:
Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively.
[Related Catalog]:
[Target]
MCP-1-CCR2b:180 nM (IC50)
[In Vitro]
Ile263 and Thr292 in CCR2 contribute significantly to binding of Teijin compound 1 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated Teijin compound 1, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with Teijin compound 1[2].
[In Vivo]
In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and Teijin compound 1 reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].
[References]
[Related Small Molecules]
INCB3344
|
Cenicriviroc
|
INCB8761(PF-4136309)
|
RS504393
|
RS-102895 hydrochloride
|
BX 471
|
TAK-779
|
Vercirnon
|
MK-0812 Succinate
|
AZD 2098
|
CCX140
|
INCB 3284
|
ZK 756326
|
CCR2-RA-[R]
|
BMS-813160
Chemical & Physical Properties
[ Molecular Formula ]:
C21H21ClF3N3O2
[ Molecular Weight ]:
439.86
[ PSA ]:
68.42000
[ LogP ]:
5.63430
[ Storage condition ]:
2-8℃