| Stereochemistry | ACHIRAL |
| Molecular Formula | C19H20N2O3 |
| Molecular Weight | 324.3737 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(OCC1=NN(CC2=CC=CC=C2)C3=C1C=CC=C3)C(O)=O
InChI
InChIKey=MTHORRSSURHQPZ-UHFFFAOYSA-N
InChI=1S/C19H20N2O3/c1-19(2,18(22)23)24-13-16-15-10-6-7-11-17(15)21(20-16)12-14-8-4-3-5-9-14/h3-11H,12-13H2,1-2H3,(H,22,23)
Bindarit (2-Methyl-2-[[1-(phenylmethyl)-1H-indazol-3yl]methoxy]propanoic acid; AF-2838) is an indazolic derivative that is devoid of any immunosuppressive effects and has no effect on arachidonic acid metabolism. It has been proved to have anti-inflammatory activity in a number of experimental diseases, including pancreatitis, arthritis, and lupus nephritis. This therapeutic effect has been associated with its ability to interfere selectively with monocyte recruitment, although the underlying molecular mechanisms are unknown. Bindarit selectively inhibits the production of the monocyte chemotactic protein subfamily of CC inflammatory chemokines (MCP-1/CCL2, MCP-3/CCL7, MCP-2/CCL8) without affecting the production of the cytokines IL-1, IL-6, or the chemokines IL-8, MIP-1α.
Approval Year
Doses
Sourcing
PubMed
Patents
Sample Use Guides
Acini were preincubated with/without bindarit (460 μM) for 30 min, and further incubated with caerulein (10−12-10−7 M) for 30 min. The dose of bindarit was chosen based on earlier reports in which it was shown to inhibit MCP-1 synthesis. Bindarit has been shown to preferentially inhibit MCP-1 production in vitro in monocytes without affecting the production of the cytokines IL-1, IL-6, or the chemokines IL-8, protein macrophage inflammatory-1alpha.
ACTIVE MOIETY
