Azilsartan
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- CAS-Nr.
- 147403-03-0
- Englisch Name:
- Azilsartan
- Synonyma:
- Azilsartan Base;2-Ethoxy-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid;Azilsartan Acid;CS-865;Tak 536;Azisartan;AZILSARTAN;AZATMint-E;Azilsartan API;Azilsartan >
- CBNumber:
- CB21090899
- Summenformel:
- C25H20N4O5
- Molgewicht:
- 456.45
- MOL-Datei:
- 147403-03-0.mol
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Azilsartan Eigenschaften
- Schmelzpunkt:
- 188 °C(dec.)
- Dichte
- 1.42
- storage temp.
- Sealed in dry,2-8°C
- L?slichkeit
- DMSO: soluble15mg/mL (clear solution)
- Aggregatzustand
- powder
- pka
- 2.05±0.10(Predicted)
- Farbe
- white to beige
- InChIKey
- KGSXMPPBFPAXLY-UHFFFAOYSA-N
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
Bildanzeige (GHS) |
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Alarmwort |
Warnung |
Gefahrenhinweise |
Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
H361 |
Kann vermutlich die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. |
Reproduktionstoxizit?t |
Kategorie 2 |
Warnung |
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P201, P202, P281, P308+P313, P405,P501 |
H413 |
Kann für Wasserorganismen sch?dlich sein, mit langfristiger Wirkung. |
Langfristig (chronisch) gew?ssergef?hrdend |
Kategorie 4 |
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Sicherheit |
P201 |
Vor Gebrauch besondere Anweisungen einholen. |
P202 |
Vor Gebrauch alle Sicherheitshinweise lesen und verstehen. |
P273 |
Freisetzung in die Umwelt vermeiden. |
P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
P308+P313 |
BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
P405 |
Unter Verschluss aufbewahren. |
P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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Azilsartan Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Azilsartan is an antagonist of the angiotensin II type 1 receptor (AT
1; IC
50 = 0.42 μM) and the active metabolite of azilsartan medoxomil . Azilsartan is formed from azilsartan medoxomil by hydrolysis in the gastrointestinal tract and liver. Azilsartan also acts as an inverse agonist, inhibiting angiotensin II-induced accumulation of inositol-1-phosphate in COS-7 cells expressing recombinant human AT
1 (IC
50 = 2.6 nM). It reduces the maximal contractile response induced by angiotensin II in isolated rabbit aortic strips (pD
2 = 9.9). Azilsartan (100 ng/kg, i.v.) inhibits the angiotensin II-induced pressor response in conscious normotensive rats.
Chemische Eigenschaften
White to Off-White Solid
Verwenden
Azilsartan is an analgesic and antiinflammatory drugs containing angiotensin II antagonists.
Definition
ChEBI: A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) f
r treatment of hypertension.
Clinical Use
Azilsartan is an orally active angiotensin II blocker which was approved and launched in Japan for
the treatment of arterial hypertension in May 2012. Azilsartan, which is marketed under the trade
name Azilva®, was discovered and developed by Takeda—the same firm which had developed and
launched a prodrug of azilsartan (azilsartan kamedoxomil, Edarbi®) in 2010. Azilsartan exhibits higher
potency and slower off-rate kinetics for type 1 angiotensin II receptors, which contributes to azilsartan’s
comparatively improved blood pressure lowering effect.
Azilsartan Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Azilsartan Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 555)Lieferanten
147403-03-0()Verwandte Suche:
- AZILSARTAN
- 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid Azilsartan
- 2-ethoxy -1- {[2'-(5-oxo-4,5-dihydro -1,2,4 -oxadiazol-3-yl) biphenyl-4-yl ] methyl} -1H –benzimi[d]dazole-7-carboxylic acid
- 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-
1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid
- 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid
- Tak 536
- Unii-F9nux55p23
- 2-ethoxy-3-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)Methyl)-3H-benzo[d]iMidazole-4-carboxylic acid
- Azilsartan 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]Methyl]benziMidazole-7-carboxylic acid
- 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl]-2-ethoxy-1H-benziMidazole-7-carboxylic Acid
- Azilsartan (TAK-536)
- AzilsartanMedoxoMilInterMediates-3
- 2. 2-Ethoxy-1-[[2'-(4,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]Methyl]benziMidazole-7-carboxylic acid
- 2-Ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl) biphenyl-4-yl]Methyl }-1H-benzo -[d]iMidazole-7- carboxylic acid
- 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-
- Azilsartan metabolite MI D4
- Azilsartan metabolite MII-D4
- Azilsartan API
- AZATMint-E
- Azilsartan, ≥98% (HPLC)
- CS-865
- Azilsartan >
- 2-Ethoxy-1-[(2-5-Oxo-4,5-Dihydro-1,2,4-Oxadiazol-3-Yl)Biphenyl-4-Yl] Methyl-1H-Benzimidazole-7-Carboxalic Biphenyl-4-Yl] Methyl-1H-Benzimidazole-7-Carboxalic Acid
- Azilsartan USP/EP/BP
- 1-[2’-(4,5-dihydro-5-oxo-4H-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]-2-ethoxy-1-H-benzimidazole-7- carboxylic acid
- 2-Ethoxy-1-[(2-5-Oxo-4,5-Dihydro-1,2,4-Oxadiazol-3-Yl)
Biphenyl-4-Yl] Methyl-1H-Benzimidazole-7-Carboxalic
Acid
- Generic API Azilsartan
- 2-Ethoxy-1-{[2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid
- Azilsartan Acid
- Azilsartan Base
- 2-Ethoxy-1-((2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid
- 2-Ethoxy-1-[[2’-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic Acid
- Azilsartan
1-[[2’-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)
[1,1’-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7- carboxylic Acid
- Azisartan
- 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylic acid
- 2-ethoxy-1-{[2'-(5-oxo-2,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid
- Azilsartan, 10 mM in DMSO
- 147403-03-0
- Intermediates
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- 147403-03-0