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Trombodipine

Names

[ CAS No. ]:
113658-85-8

[ Name ]:
Trombodipine

[Synonym ]:
2(1,1,3-trioxo-2,3-dihydro-1,2-benzisothiazol-2-yl)ethyl 2,6-dimethyl-5-(ethoxycarbonyl)-4-methyl-1,4-dihydropyridincarboxylate
2-(1,1,3-trioxo-2,3-dihydro-1,2-benzisothiazol-2-yl)ethyl 2,6-dimethyl-5-(ethoxycarbonyl)-4-methyl-1,4-dihydropyridinecarboxylate
Pca 4230
Trombodipine
3,5-Pyridinedicarboxylic acid,1,4-dihydro-2,4,6-trimethyl-,ethyl 2-(3-oxo-1,2-benzisothiazol-2(3H)-yl)ethyl ester,S,S-dioxide

Biological Activity

[Description]:

Trombodipine is an antithrombotic agent.

[Related Catalog]:

Signaling Pathways >> Others >> Others
Research Areas >> Cardiovascular Disease

[In Vitro]

Trombodipine is an antithrombotic agent. Exposure to 50 μM Trombodipine reveals an important stasis of growth. The percentage of inhibition exerted by 1 μM Trombodipine on day 3, 5 and 7 of the growth curve is 22.0±4.5, 32.0±3.0 and 29.4±6.0%, respectively (P<0.05). The inhibitory effect of Trombodipine on cell proliferation is reversible and after removal of Trombodipine the proliferation of the cells is resumed[1]. Addition of Trombodipine reduces cell number in a dose-dependent manner over a period of 4 to 6 days in culture. When compare to control cultures at the latest time points investigated, 5 μM Trombodipine decreases the number of E19P cells and human VSMCs by 25 and 21%, respectively, whereas 50 μM Trombodipine reduces E19P and human VSMC number by 85 and 74%, respectively[2].

[Cell Assay]

To estimate the proportions of cells in different phases of the cell cycle, cellular DNA contents are measured by flow cytometry. Cells are plated, allowed to attach overnight, and placed in serum-free medium for 48 h. Trombodipine (50 μM) is added at selected points during serum repletion. At the specified times after serum addition, the cells are harvested by trypsinization, washed with PBS, pelleted and resuspended in PBS containing 0.6% Nonidet P-40 and 100 μg/mL propidium iodide (PI). Flow cytometric analyses are done with a FACScan flow cytometer[1].

[References]

[1]. del Rio M, et al. Antiproliferative effects of PCA-4230, a new antithrombotic drug, in vascular smooth muscle cells. Br J Pharmacol. 1997 Apr;120(7):1360-6.


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Chemical & Physical Properties

[ Density]:
1.327g/cm3

[ Boiling Point ]:
623.2ºC at 760mmHg

[ Molecular Formula ]:
C21H24N2O7S

[ Molecular Weight ]:
448.48900

[ Flash Point ]:
330.7ºC

[ Exact Mass ]:
448.13000

[ PSA ]:
127.46000

[ LogP ]:
3.07220

[ Vapour Pressure ]:
1.88E-15mmHg at 25°C

[ Index of Refraction ]:
1.571

[ Storage condition ]:
2-8℃

Synthetic Route

Precursor & DownStream


Related Compounds

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