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
![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 Structure](CAS/GIF/138605-00-2.gif)
- CAS No.
- 138605-00-2
- Chemical 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
- Adehl;NKH 477;MKH 477;Adehl (TN);Forskolin, NKH477;Colforsin dapropate;NKH477 (hydrochloride);VIRRLEDAYYYTOD-YHEOSNBFSA-N;colforsindapropatehydrochloride;colforsin daropate hydrochloride
- CBNumber:
- CB3477436
- Molecular Formula:
- C27H44ClNO8
- Molecular Weight:
- 546.1
- MDL Number:
- MFCD00236421
- MOL File:
- 138605-00-2.mol
- MSDS File:
- SDS
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 Properties
| storage temp. | 2-8°C |
|---|---|
| solubility | H2O: soluble3mg/mL, clear to slightly hazy (warmed) |
| form | White solid |
| color | white to beige |
| Water Solubility | Soluble to 40 mM in water |
| FDA UNII | C6P4R272GT |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS06 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H300 | |||||||||
| Precautionary statements | P264-P270-P301+P310-P405-P501 | |||||||||
| Hazard Codes | T+ | |||||||||
| Risk Statements | 28 | |||||||||
| Safety Statements | 28-36/37-45 | |||||||||
| RIDADR | UN 2811 6.1 / PGII | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | AY5992600 | |||||||||
| NFPA 704 |
|
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 price More Price(15)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | N3290 | NKH 477 ≥98% (HPLC), powder | 138605-00-2 | 5mg | $147 | 2024-03-01 | Buy |
| Cayman Chemical | 11214 | NKH477 (hydrochloride) ≥95% | 138605-00-2 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 11214 | NKH477 (hydrochloride) ≥95% | 138605-00-2 | 5mg | $109 | 2024-03-01 | Buy |
| Sigma-Aldrich | N3290 | NKH 477 ≥98% (HPLC), powder | 138605-00-2 | 25mg | $581 | 2024-03-01 | Buy |
| Cayman Chemical | 11214 | NKH477 (hydrochloride) ≥95% | 138605-00-2 | 10mg | $184 | 2024-03-01 | Buy |
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,Uses,Production
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).
Definition
ChEBI: Colforsin daropate hydrochloride is the hydrochloride salt of colforsin daropate. It is a drug used for the treatment of acute heart failure. It directly stimulates adenylate cyclase and produces positive inotropic and vasodilator effects accompanied by the increase in cellular cAMP. It has a role as an adenylate cyclase agonist, an antihypertensive agent, a cardiotonic drug and a vasodilator agent. It contains a colforsin daropate(1+).
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).
storage
+4°C (desiccate)
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
Raw materials
Preparation Products
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 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| J & K SCIENTIFIC LTD. | 010-82848833 400-666-7788 | jkinfo@jkchemical.com | China | 96815 | 76 |
| 3B Pharmachem (Wuhan) International Co.,Ltd. | 821-50328103-801 18930552037 | 3bsc@sina.com | China | 15848 | 69 |
| Ascent Scientific | 4401179829988 | customerservice@ascentscientific.co.uk | United Kingdom | 279 | 60 |
| Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
138605-00-2(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)Related Search:
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