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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 Basic information |
| Product 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 | | Synonyms: | Forskolin, NKH477 - CAS 138605-00-2 - Calbiochem;Colforsin dapropate;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;VIRRLEDAYYYTOD-YHEOSNBFSA-N;y-3,4a,7,7,10a-pentamethyl-1-oxo-1h-naphtho(2,1-b)pyran-6-ylester,hydrochlor | | CAS: | 138605-00-2 | | MF: | C27H44ClNO8 | | MW: | 546.09 | | EINECS: | | Product Categories: | Signalling;Cyclic Nucleotide related | | Mol File: | 138605-00-2.mol |
| 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 Chemical Properties |
| storage temp. | 2-8°C | | solubility | H2O: soluble3mg/mL, clear to slightly hazy (warmed) | | form | White solid | | color | white to beige |
| Hazard Codes | T+ | | Risk Statements | 28 | | Safety Statements | 28-36/37-45 | | RIDADR | UN 2811 6.1 / PGII | | WGK Germany | 3 | | RTECS | AY5992600 |
| 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 Usage And Synthesis |
| Description | 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. | | Originator | Nippon Kayaku (Japan) | | Uses | 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). | | Brand name | Adele; Adehl | | Biological Activity | 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™ . | | Biochem/physiol Actions | NKH 477 is a potent, orally active adenylyl cyclase activator. It is a water soluble derivative of forskolin, and dose dependentyl increases cAMP and blocks potassium-induced contraction concetrations in smooth muscle strips (IC50 = 80 nM). NKH 477 causes relaxation of histamine treated guinea pig smooth muscle (IC50 = 32 nM). |
| 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 Preparation Products And Raw materials |
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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](/img/138605-00-2.jpg "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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