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
- 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
- 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;MKH 477;NKH 477;Adehl (TN);Forskolin, NKH477;Colforsin dapropate;NKH477 (hydrochloride);VIRRLEDAYYYTOD-YHEOSNBFSA-N;colforsindapropatehydrochloride;colforsin daropate hydrochloride
- CBNumber
- CB3477436
- Molecular Formula
- C27H44ClNO8
- Formula Weight
- 546.1
- 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 Property
- 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
Safety
- Hazard Codes
- T+
- Risk Statements
- 28
- Safety Statements
- 28-36/37-45
- RIDADR
- UN 2811 6.1 / PGII
- WGK Germany
- 3
- RTECS
- AY5992600
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H300Fatal if swallowed
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- N3290
- Product name
- NKH 477
- Purity
- ≥98% (HPLC), powder
- Packaging
- 5mg
- Price
- $147
- Updated
- 2024/03/01
- Product number
- 11214
- Product name
- NKH477 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 11214
- Product name
- NKH477 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $109
- Updated
- 2024/03/01
- Product number
- N3290
- Product name
- NKH 477
- Purity
- ≥98% (HPLC), powder
- Packaging
- 25mg
- Price
- $581
- Updated
- 2024/03/01
- Product number
- 11214
- Product name
- NKH477 (hydrochloride)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
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,Usage,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
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15848
- Advantage
- 69
- Tel
- 4401179829988
- Fax
- 4402030 700 369
- customerservice@ascentscientific.co.uk
- Country
- United Kingdom
- ProdList
- 279
- Advantage
- 60
- Tel
- 021-61415566 800-8193336
- orderCN@merckgroup.com
- Country
- China
- ProdList
- 51471
- Advantage
- 80
- Tel
- 888-539-0666
- Fax
- 888-539-0666
- info@emmx.com
- Country
- United States
- ProdList
- 8449
- Advantage
- 60
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29797
- Advantage
- 68
- Tel
- +1-781-999-5354 +1-00000000000
- marketing@targetmol.com
- Country
- United States
- ProdList
- 19892
- Advantage
- 58
- Tel
- +86-0371-86658258 15093356674;
- Fax
- 0371-86658258
- laboratory@coreychem.com
- Country
- China
- ProdList
- 30255
- Advantage
- 58
- Tel
- 86-571-88216897,88216896 13588875226
- Fax
- 86-571-88216895
- sales@hzclap.com
- Country
- CHINA
- ProdList
- 6313
- Advantage
- 58
- Tel
- 021-58447131 13564518121
- sales@dcchemicals.com
- Country
- China
- ProdList
- 9414
- Advantage
- 58