[CAS NO. 851546-61-7] PSI-697
PRODUCTS SPECIFICATIONS [851546-61-7]
DESCRIPTION [851546-61-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 367.83 |
| Molecular Formula | C21H18ClNO3 |
| SMILES | O=C(C1=C(O)C(CC2=CC=C(Cl)C=C2)=NC3=C(CCCC4)C4=CC=C13)O |
5 Publications Citing Use of MCE
Summary
PSI-697 is an oral P-selectin inhibitor with an IC 50 of 125 μM [1] .
IC50 & Target
IC50: 125 μM (P-selectin) [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 4-5 weeks male Sprague-Dawley rat (50-100 g) [1] |
| Dosage: | 0 mg/kg, 30 mg/kg, 50 mg/kg |
| Administration: | Oral administration |
| Result: | At an oral dose of 50 mg/kg reduced the number of rolling leukocytes by 39% versus vehicle control. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03860506 | Pfizer |
Healthy
|
April 1, 2008 | Phase 1 |
| NCT00367692 | Wyeth is now a wholly owned subsidiary of Pfizer |
Scleritis
|
September 2006 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 45.8 mg/mL ( 124.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7186 mL | 13.5932 mL | 27.1865 mL |
| 5 mM | 0.5437 mL | 2.7186 mL | 5.4373 mL |
| 10 mM | 0.2719 mL | 1.3593 mL | 2.7186 mL |
References
- [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.