N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE
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- CAS-Nr.
- 138605-00-2
- Englisch Name:
- N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE
- Synonyma:
- Adehl;NKH 477;MKH 477;Adehl (TN);Forskolin, NKH477;Colforsin dapropate;NKH477 (hydrochloride);VIRRLEDAYYYTOD-YHEOSNBFSA-N;colforsindapropatehydrochloride;colforsin daropate hydrochloride
- CBNumber:
- CB3477436
- Summenformel:
- C27H44ClNO8
- Molgewicht:
- 546.1
- MOL-Datei:
- 138605-00-2.mol
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N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE Eigenschaften
- storage temp.
- 2-8°C
- L?slichkeit
- H2O: soluble3mg/mL, clear to slightly hazy (warmed)
- Aggregatzustand
- White solid
- Farbe
- white to beige
- Wasserl?slichkeit
- Soluble to 40 mM in water
- InChIKey
- VIRRLEDAYYYTOD-YHEOSNBFSA-N
- SMILES
- Cl.CN(C)CCC(=O)O[C@@H]1[C@H](OC(C)=O)[C@@]2(C)O[C@](C)(CC(=O)[C@]2(O)[C@@]3(C)[C@@H](O)CCC(C)(C)[C@H]13)C=C
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Kennzeichnung gef?hrlicher |
T+ |
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| R-S?tze: |
28 |
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| S-S?tze: |
28-36/37-45 |
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| RIDADR |
UN 2811 6.1 / PGII |
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| WGK Germany |
3 |
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| RTECS-Nr. |
AY5992600 |
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| Speicherklasse |
6.1A - Combustible acute toxic Cat. 1 and 2
very toxic hazardous materials |
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| Hazard Classifications |
Acute Tox. 2 Oral |
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| Bildanzeige (GHS) |
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| Alarmwort |
Achtung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H300 |
Lebensgefahr bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 2 |
Achtung |
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P264, P270, P301+P310, P321, P330,P405, P501 |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P270 |
Bei Gebrauch nicht essen, trinken oder rauchen. |
| P301+P310 |
BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
| P405 |
Unter Verschluss aufbewahren. |
| P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Colforsin daropate was launched in Japan as a treatment for acute
heart failure. It is a water-soluble and orally active 3-dimethylaminopropionyl
(daropate) derivative of forskolin, a labdane-type diterpene isolated from the root
of Coleus forskohlii. It is obtained from forskolin in 7 steps based upon a series
of protections and deprotections of the different OH groups and a key 7,8-
transacylation. Colforsin daropate is the first in its class of adenylate cyclase
activators to be marketed in the treatment of heart failure. As forskolin, it directly
stimulates adenylate cyclase thus increasing intracellular concentration of cAMP
and inhibiting calcium mobilization. As a direct consequence, it induces a
significant vasodilatation, so provides a moderate positive inotropic and
chronotropic effect. In contrast with well-established generators of cAMP
synthesis (dobutamine), Colforsin daropate maintains its action on cardiac
muscle in the severe stage even when the beta-adrenoceptor is down-regulated
in myocardium. In several clinical trials in patients with severe congestive heart
failure (CHF), Colforsin daproate improved hemodynamic symptoms of heart
failure patients without serious adverse effects.
Verwenden
NKH 477 is a water-soluble analog of Forskolin (F701800), that is a potent activator of adenylyl cyclase, which shows some selectivity for cardiac (type V) adenylyl cyclase).
Biologische Aktivit?t
Water-soluble analog of forskolin ([3R-(3a,4ab,5b,6b,6aa,10a,10ab,10ba)]-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one ) that is a potent activator of adenylyl cyclase; shows some selectivity for cardiac (type V) adenylyl cyclase. Stimulates bronchodilation (EC 50 = 32.6 nM) and is an orally active potent positive chronotrope and hypotensive agent in vivo . Also available as part of the PKA Tocriset™ .
N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 90)Lieferanten
138605-00-2()Verwandte Suche:
- N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE
- NKH 477
- (3r-(3-alpha,4a-beta,5-beta,6-beta,6a-alpha,10-alpha,10a-beta,10b-alpha))-id
- N,N-dimethyl-, (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-yl ester b-Alanine hydrochloride
- Forskolin, NKH477
- beta-alanine,n,n-dimethyl-,5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydrox
- colforsindapropatehydrochloride
- N,N-Dimethyl-(3R,4aR,5S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-yl ester beta-alanine hydrochloride
- N,N-Dimethyl-(3R,4aR,5S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-ylesterβ-alaninehydrochloride
- NKH477 (hydrochloride)
- 6-[3-(dimethylamino)propionyl]-forskolin
- y-3,4a,7,7,10a-pentamethyl-1-oxo-1h-naphtho(2,1-b)pyran-6-ylester,hydrochlor
- N,N-Dimethyl-(3R,4aR,5S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-
- Adehl (TN)
- 1H-Naphtho[2,1-b]pyran, β-alanine deriv.
- 6-(3-Dimethylaminopropionyl)forskolin hydrochloride
- Adehl
- colforsin daropate hydrochloride
- β-Alanine, N,N-dimethyl-, (3R,4aR,5S,6S,6aS,10S,10aR,10bS)-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-yl ester, hydrochloride
- β-Alanine, N,N-dimethyl-, 5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho[2,1-b]pyran-6-yl ester, hydrochloride, [3R-(3α,4aβ,5β,6β,6aα,10α,10aβ,10bα)]-
- MKH 477
- Forskolin, NKH477 - CAS 138605-00-2 - Calbiochem
- Colforsin dapropate
- VIRRLEDAYYYTOD-YHEOSNBFSA-N
- NKH 477 (Colforsin daropate), an adenylyl cyclase activator
- 138605-00-2
- C27H43NO8HCl
- C27H44ClNO8
- Signalling
- Cyclic Nucleotide related
