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851546-61-7

851546-61-7 structure
851546-61-7 structure
  • Name: PSI-697
  • Chemical Name: 2-[(4-chlorophenyl)methyl]-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid
  • CAS Number: 851546-61-7
  • Molecular Formula: C21H18ClNO3
  • Molecular Weight: 367.82600
  • Catalog: Research Areas Cancer
  • Create Date: 2016-02-09 08:13:32
  • Modify Date: 2024-01-06 17:19:10
  • PSI-697is a P-selectin inhibitor.In vivo: 30 mg/kg; oral gavage daily. Animals treaed with PSI-697 shows a significantly decreased intimal thickness score when compared with vehicle control IVCs. PSI-697 significantly decreased vein wall levels of platelet-derived growth factor . d PSI-697 inhibits vein wall injury independently of thrombus mass. P-selectin inhibition seemed superior to LMWH in measured parameters of injury and mediator inhibition. PSI-697 inhibit vein wall injury independently of thrombus size in a rodent model of DVT. [1] PSI-697 (50 mg/kg p.o.) significantly reduced the number of rolling leukocytes by 39% (P < 0.05) versus vehicle control. In a rat venous thrombosis model, PSI-697 (100 mg/kg p.o.) reduced thrombus weight by 18% (P < 0.05) relative to vehicle, without prolonging bleeding time. [2] Animals receiving PSI-697 demonstrated significantly increased plasma D-dimer levels versus LMWH and control animals six hours post thrombus induction.[3]

Name 2-[(4-chlorophenyl)methyl]-3-hydroxy-7,8,9,10-tetrahydrobenzo[h]quinoline-4-carboxylic acid
Synonyms 2-(4-Chloro-benzyl)-3-hydroxy-7,8,9,10-tetrahydro-benzo[h]quinoline-4-carboxylic acid
UNII-LH1XC916ME
PSI-697
Description PSI-697is a P-selectin inhibitor.In vivo: 30 mg/kg; oral gavage daily. Animals treaed with PSI-697 shows a significantly decreased intimal thickness score when compared with vehicle control IVCs. PSI-697 significantly decreased vein wall levels of platelet-derived growth factor . d PSI-697 inhibits vein wall injury independently of thrombus mass. P-selectin inhibition seemed superior to LMWH in measured parameters of injury and mediator inhibition. PSI-697 inhibit vein wall injury independently of thrombus size in a rodent model of DVT. [1] PSI-697 (50 mg/kg p.o.) significantly reduced the number of rolling leukocytes by 39% (P < 0.05) versus vehicle control. In a rat venous thrombosis model, PSI-697 (100 mg/kg p.o.) reduced thrombus weight by 18% (P < 0.05) relative to vehicle, without prolonging bleeding time. [2] Animals receiving PSI-697 demonstrated significantly increased plasma D-dimer levels versus LMWH and control animals six hours post thrombus induction.[3]
Related Catalog
References

[1]. 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.

[2]. 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.

[3]. 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.

Molecular Formula C21H18ClNO3
Molecular Weight 367.82600
Exact Mass 367.09800
PSA 70.42000
LogP 4.76160
Storage condition 2-8℃

~39%

851546-61-7 structure

851546-61-7

Literature: Wang, Youchu Patent: US2007/82923 A1, 2007 ; Location in patent: Page/Page column 12 ;

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851546-61-7 structure

851546-61-7

Literature: Wyeth Patent: US2005/101569 A1, 2005 ; Location in patent: Page/Page column 14 ;

~41%

851546-61-7 structure

851546-61-7

Literature: Kaila, Neelu; Janz, Kristin; Huang, Adrian; Moretto, Alessandro; DeBernardo, Silvano; Bedard, Patricia W.; Tam, Steve; Clerin, Valerie; Keith Jr., James C.; Tsao, Desiree H.H.; Sushkova, Natalia; Shaw, Gray D.; Camphausen, Raymond T.; Schaub, Robert G.; Wang, Qin Journal of Medicinal Chemistry, 2007 , vol. 50, # 1 p. 40 - 64

~%

851546-61-7 structure

851546-61-7

Literature: Kaila, Neelu; Janz, Kristin; Huang, Adrian; Moretto, Alessandro; DeBernardo, Silvano; Bedard, Patricia W.; Tam, Steve; Clerin, Valerie; Keith Jr., James C.; Tsao, Desiree H.H.; Sushkova, Natalia; Shaw, Gray D.; Camphausen, Raymond T.; Schaub, Robert G.; Wang, Qin Journal of Medicinal Chemistry, 2007 , vol. 50, # 1 p. 40 - 64

~%

851546-61-7 structure

851546-61-7

Literature: Kaila, Neelu; Janz, Kristin; Huang, Adrian; Moretto, Alessandro; DeBernardo, Silvano; Bedard, Patricia W.; Tam, Steve; Clerin, Valerie; Keith Jr., James C.; Tsao, Desiree H.H.; Sushkova, Natalia; Shaw, Gray D.; Camphausen, Raymond T.; Schaub, Robert G.; Wang, Qin Journal of Medicinal Chemistry, 2007 , vol. 50, # 1 p. 40 - 64

~%

851546-61-7 structure

851546-61-7

Literature: Kaila, Neelu; Janz, Kristin; Huang, Adrian; Moretto, Alessandro; DeBernardo, Silvano; Bedard, Patricia W.; Tam, Steve; Clerin, Valerie; Keith Jr., James C.; Tsao, Desiree H.H.; Sushkova, Natalia; Shaw, Gray D.; Camphausen, Raymond T.; Schaub, Robert G.; Wang, Qin Journal of Medicinal Chemistry, 2007 , vol. 50, # 1 p. 40 - 64