| Bioactivity | PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[1]. | ||||||||||||
| Target | IC50: 125 μM (P-selectin) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | PSI-697 | ||||||||||||
| CAS | 851546-61-7 | ||||||||||||
| Formula | C21H18ClNO3 | ||||||||||||
| Molar Mass | 367.83 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |