TAS 301
TAS 301 structure
|
Common Name | TAS 301 | ||
|---|---|---|---|---|
| CAS Number | 193620-69-8 | Molecular Weight | 357.402 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 573.2±50.0 °C at 760 mmHg | |
| Molecular Formula | C23H19NO3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 300.5±30.1 °C | |
Use of TAS 301TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF. |
| Name | 3-[bis(4-methoxyphenyl)methylidene]-1H-indol-2-one |
|---|---|
| Synonym | More Synonyms |
| Description | TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF. |
|---|---|
| Related Catalog | |
| Target |
PKC |
| In Vitro | TAS-301 (1-10 μM) concentration-dependently inhibits PKC activation and Ca2+ influx, induced by PDGF, with 62.7% inhibition on PKC activation at 10 μM, and reduces PMA-induced AP-1, with 38% and 67.6% inhibition at 3 and 10 μM, respectively[1]. TAS-301 (0.3-3 μM) dose-dependently reduces the migration of cells induced by growth factors (PDGF-BB, IGF-1,HB-EGF). TAS-301 (1-10 μM) also decreases bFGF-induced BrdU incorporation, especially at 3 and 10 μM[2]. |
| In Vivo | TAS-301 (3-100 mg/kg, p.o.) dose-dependently reduces the neointimal thickening and I/M ratio and decreases the level of intimal cells in rats 14 days after balloon injury[2]. |
| Cell Assay | Cell proliferation is determined by the incorporation of BrdU by quiescent cells. SMCs are seeded at 1 × 104cells/well in 96-well plates in DMEM containing 10% FBS. Two days after the seeding, their growth is arrested for 3 days in a serum-free DMEM containing 5 μg/mL insulin, 5 μg/mL transferrin and 5 ng/mL sodium selenium (ITS). Then, the DMEM/ITS is removed, and serum-free DMEM containing 0.1% BSA with or without TAS-301 or tranilast is added to the quiescent cells 2 hr before treatment with the growth factor (i.e., bFGF 0.1 ng/mL). At 24 hr after stimulation, BrdU (10 μM) is added to the cells; 24 hr later, the cells are fixed. An ELISA is used to detect and to quantify the incorporated BrdU (n = 6). The drugs are present during the entire experiment[2]. |
| Animal Admin | Rats[2] On the 14th day after the balloon injury, the rats are anesthetized with ether so as to avoid any stress to the animals and then perfused transcardially with saline, followed by 10% buffered formalin. Next, the left carotid artery (length from aortic arch to bifurcation) is removed, postfixed and embedded in paraffin. Then, 3-μm-thick artery sections (six sections for each artery) are cut and stained with hematoxylin and eosin. The cross-sectional areas of the intima and the media on photographs are measured by use of a digital analyzer. The average of the ratio of the intimal area to the medial area in each artery is determined. Experimental groups are as follows: Vehicle (n = 9), TAS-301 (3, 10, 30 and 100 mg/kg,n = 9) and tranilast (100 and 300 mg/kg,n = 9). The data on two rats (one in TAS-301 100 mg/kg group and one in tranilast 100 mg/kg group) is omitted from the evaluation because of death due to faulty oral administration[2]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 573.2±50.0 °C at 760 mmHg |
| Molecular Formula | C23H19NO3 |
| Molecular Weight | 357.402 |
| Flash Point | 300.5±30.1 °C |
| Exact Mass | 357.136505 |
| PSA | 47.56000 |
| LogP | 4.72 |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.630 |
| Storage condition | 2-8℃ |
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Safety Phrases | 22-24/25 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
|
TAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries.
J. Pharmacol. Exp. Ther. 285 , 1280-1286, (1998) The purpose of this study was to determine the efficacy and the possible mechanism of action of a recently synthesized drug, TAS-301 [3-bis (4-methoxyphenyl)methylene-2-indolinone], on intimal formati... |
|
|
TAS-301 blocks receptor-operated calcium influx and inhibits rat vascular smooth muscle cell proliferation induced by basic fibroblast growth factor and platelet-derived growth factor.
Jpn. J. Pharmacol. 84(3) , 252-8, (2000) The purpose of this study was to determine the effect of a recently synthesized drug, TAS-301 [3-bis(4-methoxyphenyl)methylene-2-indolinone], on vascular smooth muscle cell (VSMC) proliferation and th... |
|
|
Tas-301, a new synthetic inhibitor of neointimal thickening after balloon injury, inhibits calcium-dependent signal transduction and cytoskeletal reorganization.
Pharmacology 63 , 17-27, (2001) We previously demonstrated that a recently synthesized drug, TAS-301 [3-bis(4-methoxyphenyl)methylene-2-indolinone], inhibited neointimal thickening after single-balloon injury to the rat common carot... |
| TAS-301 |
| 3-[Bis(4-methoxyphenyl)methylene]-1,3-dihydro-2H-indol-2-one |
| 2H-Indol-2-one, 3-[bis(4-methoxyphenyl)methylene]-1,3-dihydro- |
| IN1440 |
| 3-Bis-(4-methoxphenyl)methylene-2-indolinone |
| 3-bis(4-Methoxyphenyl)methylene-2-indolinone |