DIBENZAZEPINE
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- CAS-Nr.
- 209984-56-5
- Englisch Name:
- DIBENZAZEPINE
- Synonyma:
- DBZ (Dibenzazepine);Dibenzazepine (YO-01027);GSI-XX;CS-366;YO01027;DIBENZAZEPINE;Deshydroxy LY-411575;6-Chloro-α-Tetralone;YO-01027, 10 mM in DMSO;γ-Secretase Inhibitor XX
- CBNumber:
- CB11234300
- Summenformel:
- C26H23F2N3O3
- Molgewicht:
- 463.48
- MOL-Datei:
- 209984-56-5.mol
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DIBENZAZEPINE Eigenschaften
- Schmelzpunkt:
- 257-259C
- Siedepunkt:
- 801.3±65.0 °C(Predicted)
- Dichte
- 1.35
- storage temp.
- -20°C
- L?slichkeit
- DMSO: soluble15mg/mL, clear
- pka
- 12.76±0.20(Predicted)
- Aggregatzustand
- White solid
- Farbe
- white to beige
- Optische Rotation
- [α]/D -128.0 to -154.0°-0.25 in methanol
- InChIKey
- QSHGISMANBKLQL-OWJWWREXSA-N
- SMILES
- Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)N[C@H]2c3c(cccc3)c4c(cccc4)N(C2=O)C)F
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
Xi |
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| R-S?tze: |
36/37/38 |
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| S-S?tze: |
26 |
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| WGK Germany |
3 |
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| HS Code |
29337900 |
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| Speicherklasse |
11 - Combustible Solids |
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| Hazard Classifications |
Acute Tox. 4 Oral
Skin Sens. 1A |
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| Bildanzeige (GHS) |
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| Alarmwort |
Warnung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| 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. |
| P321 |
Besondere Behandlung |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P362 |
Kontaminierte Kleidung ausziehen und vor erneutem Tragen waschen. |
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DIBENZAZEPINE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
γ-
Secretase is a multi-
subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-
cadherin, and ErbB4. The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39-
to 42-
amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease. DBZ is a dipeptidic inhibitor of γ-
secretase that potently blocks the cleavage of Notch into its active signaling effector, Notch intracellular domain, in human T cell lymphoma (SupT1) cells (IC
50 = 1.7 nM). Within 4 hours after a single 100 μM/kg dose, DBZ demonstrates anti-
Alzheimer activity in an APP transgenic mouse model characterized by high levels of Aβ40 by reducing Aβ40 levels by 71%.
Chemische Eigenschaften
White Solid
Verwenden
DIBENZAZEPINE is a dipeptidic-secretase inhibitor and a antiAlzheimer agent.
Allgemeine Beschreibung
A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ
40 levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 μmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC
50 = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and
ApcMin mouse models (10 μmol/kg, i.p).
DIBENZAZEPINE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
DIBENZAZEPINE Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 179)Lieferanten
- DIBENZAZEPINE
- N-[(1S)-2-[[(7S)-6,7-Dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluorobenzeneacetamide
- Dibenzazepine (Deshydroxy LY 411575)
- YO01027
- γ-Secretase Inhibitor XX
- YO-01027/Dibenzazepine/LY 411575
- (2S)-2-[2-(3,5-Difluorophenyl)acetaMide]-N-[(7S)-5-Methyl-6-oxo-6,7-dihydro-5H-dibenzo[B,D]azepin-7-
- (S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7
- YO-01027 (Dibenzazepine)
- (S)-2-(2-(3,5-Difluorophenyl)acetamido)-N-((S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepi
- 7-(S)-[N'(3,5-difluorophenylacetyl)-L-alaninyl]amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one
- (S,S)-2-[2-(3,5-Difluorophenyl)acetylamino]-N-(5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)propionamide
- Deshydroxy LY-411575
- GSI-XX
- γ-Secretase Inhibitor DBZ
- Dibenzazepine (deshydroxy LY 411575) DBZ
- Dibenzazepine, 98%, γ-secretase inhibitor
- YO-01027; YO01027; DIBENZAZEPINE; DESHYDROXY LY 411575;DBZ
- CS-366
- DBZ, γ-Secretase Inhibitor
- γ-Secretase Inhibitor XX - CAS 209984-56-5 - Calbiochem
- YO-01027 (Dibenzazepine, DBZ)
- gamma-Secretase Inhibitor XX
- Benzeneacetamide, N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-
- 6-Chloro-α-Tetralone
- γ-secretase,YO 01027,Gamma secretase,Notch,YO-01027,inhibit,YO01027,Inhibitor
- Dibenzazepine，LY-411575/Deshydroxy LY-411575
- YO-01027, 10 mM in DMSO
- γ-Secretase Inhibitor XX
- DBZ (Dibenzazepine)
- Dibenzazepine (YO-01027)
- 209984-56-5
- C26H23F2N3O3
- Inhibitor
- Inhibitors
- Intermediates & Fine Chemicals
- Pharmaceuticals
- A dipeptidic (c)-secretase inhibitor and anti-Alzheimer agent.
- All Inhibitors
