TAS-301

Cas：193620-69-8

Product Information：

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.

Chemical Formula: C23H19NO3

Exact Mass: 357.13649

Molecular Weight: 357.41

Elemental Analysis: C, 77.29; H, 5.36; N, 3.92; O, 13.43

Chemical Name:

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

InChi Key:

KUEYYIJXBRWZIB-UHFFFAOYSA-N

InChi Code: 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)

Smiles Code:

O=C1NC2=C(C=CC=C2)/C1=C(C3=CC=C(OC)C=C3)\C4=CC=C(OC)C=C4

Technical Data：

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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, Shimooka T, Takeichi Y, Azuma M, Houchi H, Minakuchi K. Improvement of solubility and oral bioavailability of a poorly water-soluble drug, TAS-301, by its melt-adsorption on a porous calcium silicate. J Pharm Sci. 2002 Feb;91(2):362-70. PubMed PMID: 11835196.

3. Sasaki E, Miyoshi K, Nozawa Y, Kanda A, Nakano K, Yamasaki Y, Miyake H, Matsuura N. Tas-301, a new synthetic inhibitor of neointimal thickening after balloon injury, inhibits calcium-dependent signal transduction and cytoskeletal reorganization. Pharmacology. 2001 Jul;63(1):17-27. PubMed PMID: 11408828.

4. Sasaki E, Nozawa Y, Miyoshi K, Kanda A, Yamasaki Y, Miyake H, Matsuura N. 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. 2000 Nov;84(3):252-8. PubMed PMID: 11138725.

5. 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.