For research use only. Not for therapeutic Use.
PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[1].
PSI-697 inhibits the binding of a soluble human P-selectin to PSGL-1, in a reproducible concentration-dependent manner inhibiting 50% of binding at a concentration of 125 μM in vitro[1].
PSI-697 (0-50 mg/kg; p.o.) significantly reduces the number of rolling leukocytes by 39% versus vehicle control[1].
PSI-697 (100 mg/kg; p.o.) reduces thrombus weight by 18% relative to vehicle, without prolonging bleeding time in a rat venous thrombosis model[1].
PSI-697 (30 mg/kg; p.o.; daily; 6 days) promotes thrombus resolution and decreases inflammation in a baboon model of venous thrombosis[2].
PSI-697 ((30 mg/kg; i.g.; daily) decreases vein wall injury in a rat stenosis model of venous thrombosis[2].
| Catalog Number | I005108 |
| CAS Number | 851546-61-7 |
| Synonyms | 2-[(4-chlorophenyl)methyl]-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid |
| Molecular Formula | C21H18ClNO3 |
| Purity | ≥95% |
| InChI | InChI=1S/C21H18ClNO3/c22-14-8-5-12(6-9-14)11-17-20(24)18(21(25)26)16-10-7-13-3-1-2-4-15(13)19(16)23-17/h5-10,24H,1-4,11H2,(H,25,26) |
| InChIKey | DIEPFYNZGUUVHD-UHFFFAOYSA-N |
| SMILES | C1CCC2=C(C1)C=CC3=C(C(=C(N=C23)CC4=CC=C(C=C4)Cl)O)C(=O)O |
| Reference | [1]. Bedard PW et al. Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther. [2]. Myers DD Jr et al. Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation. Thromb Haemost. 2007 Mar;97(3):400-7. [3]. Myers DD Jr et al. Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis. J Vasc Surg. 2006 Sep;44(3):625-32. |
