BMY 42393
BMY 42393 Basic information
- Product Name:
- BMY 42393
- Synonyms:
-
- BMY 42393
- Acetic acid, 2-[3-[2-(4,5-diphenyl-2-oxazolyl)ethyl]phenoxy]-
- CAS:
- 136451-58-6
- MF:
- C25H21NO4
- MW:
- 399.44
- Mol File:
- 136451-58-6.mol
BMY 42393 Chemical Properties
- Boiling point:
- 579.9±50.0 °C(Predicted)
- Density
- 1.230±0.06 g/cm3(Predicted)
- pka
- 3.18±0.10(Predicted)
BMY 42393 Usage And Synthesis
Description
BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. BMY 42393 competed for radiolabeled iloprost and PGE1 binding to platelet membranes (IC50; 170 nM and 130 nM, respectively).
Uses
BMY 42393 is an orally active prostacyclin agonist which suppresses monocyte-macrophage atherogenic activity and cytokine production. BMY 42393 can be used for atherosclerosis research[1].
in vivo
BMY 42393 (30 mg/kg/d, diet, 10 weeks) inhibits mononuclear cell adhesion by 35%, decreases foam cells per square millimeter by 44%, reduces foam cell size by 26%, reduces fatty streak area by 40%, and decreases intimal oil red O staining by 39% in hamsters received a mild atherogenic diet[1].
References
[1] Kowala MC, et al. Prostacyclin agonists reduce early atherosclerosis in hyperlipidemic hamsters. Octimibate and BMY 42393 suppress monocyte chemotaxis, macrophage cholesteryl ester accumulation, scavenger receptor activity, and tumor necrosis factor production. Arterioscler Thromb. 1993 Mar;13(3):435-44. DOI:10.1161/01.atv.13.3.435