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
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)
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
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.
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.
- 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.
- 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.
- 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.
- 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.
- 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.
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