| Identification | Back Directory | [Name]
P-Selectin Inhibitor | [CAS]
851546-61-7 | [Synonyms]
PSI-697
PSI 697,PSI697
P-Selectin Inhibitor
Benzo[h]quinoline-4-carboxylic acid, 2-[(4-chlorophenyl)methyl]-7,8,9,10-tetrahydro-3-hydroxy- | [Molecular Formula]
C21H18ClNO3 | [MDL Number]
MFCD09832577 | [MOL File]
851546-61-7.mol | [Molecular Weight]
367.83 |
| Chemical Properties | Back Directory | [Boiling point ]
553.0±50.0 °C(Predicted) | [density ]
1.383±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: ≥ 45.8 mg/mL (124.51 mM) | [form ]
Solid | [pka]
0.89±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[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: | 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. |
| [storage]
Store at -20°C | [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. DOI:10.1124/jpet.107.128124
[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. PMID:17334507
[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. DOI:10.1016/j.jvs.2006.05.021 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|