TAS-301

TAS-301 is a potent and selective constrictive remodeling regulator on renarrowing after balloon overstretch injury of porcine coronary artery. TAS-103 inhibits smooth muscle cell migration and proliferation. TAS-103 inhibits intimal thickening after balloon injury to rat carotid arteries. 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. TAS-103 inhibits calcium-dependent signal transduction and cytoskeletal reorganization.

Product information

CAS Number: 193620-69-8

Molecular Weight: 357.40

Formula: C23H19NO3

Chemical Name: 3-[Bis(4-methoxyphenyl)methylene]-1,3-dihydro-2H-indol-2-one

Smiles: COC1C=CC(=CC=1)C(=C1C(=O)NC2=CC=CC=C21)C1C=CC(=CC=1)OC

InChiKey: KUEYYIJXBRWZIB-UHFFFAOYSA-N

InChi: InChI=1S/C23H19NO3/c1-26-17-11-7-15(8-12-17)21(16-9-13-18(27-2)14-10-16)22-19-5-3-4-6-20(19)24-23(22)25/h3-14H,1-2H3,(H,24,25)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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. 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.

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.

References:

1. Kinoshita M, Baba K, Nagayasu A, Yamabe K, Azuma M, Houchi H, Minakuchi K. Highly stabilized amorphous 3-bis(4-methoxyphenyl)methylene-2-indolinone (TAS-301) in melt-adsorbed products with silicate compounds. Drug Dev Ind Pharm. 2003 May;29(5):523-9. PubMed PMID: 12779282.
2. Kinoshita M, Baba K, Nagayasu A, Yamabe K, Azuma M, Houchi H, Minakuchi K. Highly stabilized amorphous 3-bis(4-methoxyphenyl)methylene-2-indolinone (TAS-301) in melt-adsorbed products with silicate compounds. Drug Dev Ind Pharm. 2003 May;29(5):523-9. PubMed PMID: 12779282.
3. Sasaki E, Tanahashi Y, Yamasaki Y, Oda N, Nozawa Y, Terakawa H, Miyoshi K, Muranaka Y, Miyake H, Matsuura N. Inhibitory effect of TAS-301, a new synthesized constrictive remodeling regulator, on renarrowing after balloon overstretch injury of porcine coronary artery. J Pharmacol Exp Ther. 2000 Dec;295(3):1043-50. PubMed PMID: 11082439.

Products are for research use only. Not for human use.