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PHENSERINE

PHENSERINE Struktur
101246-66-6
CAS-Nr.
101246-66-6
Englisch Name:
PHENSERINE
Synonyma:
PHENSERINE;(-)-Phenserine;(3as-cis)-amate(ester;(-)-Eseroline phenylcarbamate;(-)-Eseroline phenylcarbamate;(-)-N-PHENYLCARBAMOYLESEROLINE;3-b)indol-5-ol,1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-pyrrolo(phenylcarb;1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-pyrrolo[2,3-b]indol-5-ol phenylcarbamate (ester);(3aS,8aR)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol5-(N-phenylcarbamate);Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(N-phenylcarbamate), (3aS,8aR)-
CBNumber:
CB5731231
Summenformel:
C20H23N3O2
Molgewicht:
337.42
MOL-Datei:
101246-66-6.mol

PHENSERINE Eigenschaften

Schmelzpunkt:
151-152 °C
Siedepunkt:
468.7±45.0 °C(Predicted)
Dichte
1.228±0.06 g/cm3(Predicted)
storage temp. 
2-8°C
L?slichkeit
H2O: <2mg/mL
Aggregatzustand
solid
pka
13.05±0.70(Predicted)
Farbe
off-white
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher Xi
R-S?tze: 36/37/38
S-S?tze: 26
WGK Germany  3
RTECS-Nr. UY8586000
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P271 Nur im Freien oder in gut belüfteten R?umen verwenden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.

PHENSERINE Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Phenserine is inhibitor of amyloid precursor protein (APP). Used in Alzheimer’s treatments.

Biologische Aktivit?t

Physostigmine analog that inhibits acetylcholinesterase. Inhibits production of amyloid precursor protein (APP) and A β . Improves morris water maze performance of scopolamine-treated rats.

Enzyminhibitor

This long-acting AChE inhibitor and A?42-lowering agent (FW = 337,42 g/mol; CAS 101246-66-6), also known as (–) -N-phenylcarbamoyl eseroline, is a carbamate analogue of eserine (or physostigmine) that inhibits acetylcholinesterase and is under active investigation for its potential in cholinomimetic therapy to reduce cognitive impairments associated with aging and Alzheimer's Disease. Phenserine is a potent and highly selective AChE inhibitor (IC50 = 22 nM), displaying 70x greater inhibitory action than observed with butyrylcholinesterase, or BChE (IC50 = 1560 nM), both in vitro and in clinical trials for treatment of Alzheimer's disease (1-5). Compared to physostigmine and tacrine, phenserine appears to be less toxic and robustly enhances cognition in animal models. In rats, phenserine achieves maximum acetylcholinesterase inhibition of 73.5% at 5 min, maintaining high and relatively constant inhibition for >8 hours. Phenserine decreased the levels of secreted b-amyloid precursor protein (b- APP) in the cerebrospinal fluid (CSF) of forebrain cholinergic system- lesioned rats, whereas DFP, a relatively non-specific cholinesterase inhibitor, failed to affect CSF levels of secreted b-APP. Such findings suggest that phenserine alters the induction of cortical b-APP mRNAs and increased levels of secreted b-APP in the CSF. Phenserine reduces Ab levels by regulating b-APP translation via a recently described iron regulatory element in the 5'-untranslated region of b-APP mRNA that was previously shown to be up-regulated in the presence of interleukin-1. Other dual AChE/A?42 inhibitors include: rivastigmine, ladostigil, asenapine, phenserine, amitriptyline, clomipramine, doxepin and desipramine. Posiphen, the better-tolerated (+) -enantiomer of phenserine, is devoid of anticholinesterase action, but represses translation of neural α- synuclein, a druggable target in the treatment of Parkinson Disease.

PHENSERINE Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


PHENSERINE Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 41)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 32161 58
Nextpeptide Inc
+86-0571-81612335 +8613336028439
sales@nextpeptide.com China 19908 58
Alfa Chemistry

Info@alfa-chemistry.com United States 24072 58
SUZHOU SENFEIDA CHEMICAL CO.,LTD
+86-0512-83500002 +8615195660023
sales@senfeida.com China 23046 58
Aladdin Scientific
+1-+1(833)-552-7181
sales@aladdinsci.com United States 52924 58
Shanghai Eyougene biotechnology development co.LTD 021-52277372 13564545227
dom.sales@eyougene.com China 245 58
3B Pharmachem (Wuhan) International Co.,Ltd. 821-50328103-801 18930552037
3bsc@sina.com China 15839 69
Chemsky (shanghai) International Co.,Ltd 021-50135380
shchemsky@sina.com China 15402 60
Hangzhou Yuhao Chemical Technology Co., Ltd 0571-82693216
info@yuhaochemical.com China 9387 52
EMMX Biotechnology LLC 888-539-0666
info@emmx.com United States 8447 60

101246-66-6()Verwandte Suche:


  • (3as-cis)-amate(ester
  • 3-b)indol-5-ol,1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-pyrrolo(phenylcarb
  • (-)-N-PHENYLCARBAMOYLESEROLINE
  • PHENSERINE
  • (3aS,8aR)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol5-(N-phenylcarbamate)
  • 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-pyrrolo[2,3-b]indol-5-ol phenylcarbamate (ester)
  • (-)-Eseroline phenylcarbamate
  • Pyrrolo[2,3-b]indol-5-ol, 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethyl-, 5-(N-phenylcarbamate), (3aS,8aR)-
  • (-)-Phenserine
  • (-)-Eseroline phenylcarbamate
  • 101246-66-6
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