193620-69-8
193620-69-8 structure
- Name: TAS 301
- Chemical Name: 3-[bis(4-methoxyphenyl)methylidene]-1H-indol-2-one
- CAS Number: 193620-69-8
- Molecular Formula: C23H19NO3
- Molecular Weight: 357.402
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-06-20 15:43:22
- Modify Date: 2024-01-08 15:47:25
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TAS-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 |
|---|---|
| Synonyms |
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 |
| 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 |