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8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione

8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione Struktur
155270-99-8
CAS-Nr.
155270-99-8
Englisch Name:
8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione
Synonyma:
CS-285;KW-6002;Itofylline;Itraphylline;stradefylline;istradefylline;10mg 50mg 100mg 1g 5g;Istradefylline-13C-d3;KW6002/Istradefylline;Istradefylline (KW-6002)
CBNumber:
CB11261287
Summenformel:
C20H24N4O4
Molgewicht:
384.43
MOL-Datei:
155270-99-8.mol

8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione Eigenschaften

Schmelzpunkt:
191 °C
Siedepunkt:
601.0±65.0 °C(Predicted)
Dichte
1.24±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
DMSO: soluble5mg/mL (clear solution)
Aggregatzustand
powder
pka
0.47±0.70(Predicted)
Farbe
white to beige
InChIKey
IQVRBWUUXZMOPW-PKNBQFBNSA-N
CAS Datenbank
155270-99-8
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher T
R-S?tze: 25
S-S?tze: 45
RIDADR  UN 2811 6.1 / PGIII
WGK Germany  3
HS Code  2933.99.7500
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H301 Giftig bei Verschlucken. Akute Toxizit?t oral Kategorie 3 Achtung GHS hazard pictogramssrc="/GHS06.jpg" width="20" height="20" /> P264, P270, P301+P310, P321, P330,P405, P501
Sicherheit
P301+P310 BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.

8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

In March 2013, istradefylline (also known as KW-6002) was approved in Japan for adjunctive treatment of Parkinson’s disease (PD). Istradefylline acts by antagonism of the adenosine A2A receptor, which is colocalized with dopamine D2 receptors in the striatum, to enhance dopamine D2-dependent signaling. Istradefylline is a light-sensitive compound and has been evaluated in vitro under low-light conditions to prevent isomerization of the (E)-styryl group and decomposition. Istradefylline has a Ki of 2.2 nM for the rat adenosine A2A receptor and an ED50 of 0.03 mg/kg, po, in reversal of haloperidol-induced catalepsy in mice. Further characterization showed istradefylline to have a Ki of 12 nM for the human adenosine A2A receptor, to be highly selective, and to be a functional competitive antagonist. Istradefylline has activity alone and in combination with levo-dopa in preclinical animal models of PD. The synthesis of istradefylline was accomplished by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide-mediated coupling of 5,6-diamino-1,3-diethyluracil with 3,4-dimethoxycinnamic acid, followed by cyclization upon treatment with aqueous NaOH, and selective methylation (MeI, K2CO3, and DMF).

Verwenden

Treatment of Parkinson’s disease (adenosine A 2A receptor antagonist).

8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 229)Lieferanten
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155270-99-8()Verwandte Suche:

  • 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione
  • istradefylline
  • KW-6002
  • 10mg 50mg 100mg 1g 5g
  • (E)-8-(3,4-diMethoxystyryl)-1,3-diethyl-7-Methyl-1H-purine-2,6(3H,7H)-dione
  • 8-[(E)-2-(3,4-diMethoxyphenyl)ethenyl]-1,3-diethyl-7-Methyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione
  • Istradefylline (KW-6002)
  • 1H-Purine-2,6-dione,8-[(1E)-2-(3,4-diMethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-Methyl-
  • Istradefylline 8-[(E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methylpurine-2,6-dione
  • (E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methylxanthine
  • 8-[(1E)-2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
  • (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purin-2,6-dione
  • Itraphylline
  • Istradefylline-13C-d3
  • CS-285
  • 8-[(1E)-2-(2-(3,4-Dimethoxyphenyl)ethenyl]-1,3-diethyl-3,7-dihydro-7-methyl-1H-purine-2,6-dione
  • 8-[(E)-2-(3,4-DIMETHOXYPHENYL)ETHENYL]-1,3-DI...
  • 8-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]-1,3-diethyl-7-methyl-purine-2,6 -dione USP/EP/BP
  • Itraphylline impurities867
  • stradefylline
  • Itraphylline impurities5
  • 2-dioleoyl-sn-glycero-3-phosphocholine
  • KW6002/Istradefylline
  • (E)-8-(3,4-Dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione
  • Itofylline
  • 155270-99-8
  • Inhibitors
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