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PKC&ROCK

TAS-301 (193620-69-8)

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF….

Not Intended for Therapeutic Use. For research use only.

CAS: 193620-69-8 Category

TAS-301 (193620-69-8) Description

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.

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.

TAS-301 (193620-69-8) Specifications

Product Name TAS-301
Synonym TAS-301, TAS30
Chemical Name 3-[Bis(4-methoxyphenyl)methylene]-1,3-dihydro-2H-indol-2-one
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 193620-69-8
Molecular Formula C23H19NO3
Molecular Weight 357.41
Monoisotopic Mass 357.13649 g/mol
MDL number MFCD05865245
InChIKey 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 O=C1NC2=C(C=CC=C2)/C1=C(C3=CC=C(OC)C=C3)\C4=CC=C(OC)C=C4
Form Solid powder
Color Yellow
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and light
Application An inhibitor of smooth muscle cell migration and proliferation

 


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RIDADR NONH for all modes of transport

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.

1 review for TAS-301 (193620-69-8)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The TAS-301 (193620-69-8) is high purity,also customer service is pretty nice !gotta try!!

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