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Details

Stereochemistry ABSOLUTE
Molecular Formula C27H43NO8.ClH
Molecular Weight 546.093
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of COLFORSIN DAROPATE HYDROCHLORIDE

SMILES

Cl.[H][C@@]12[C@H](OC(=O)CCN(C)C)[C@H](OC(C)=O)[C@@]3(C)O[C@](C)(CC(=O)[C@]3(O)[C@@]1(C)[C@@H](O)CCC2(C)C)C=C

InChI

InChIKey=VIRRLEDAYYYTOD-YHEOSNBFSA-N
InChI=1S/C27H43NO8.ClH/c1-10-24(5)15-18(31)27(33)25(6)17(30)11-13-23(3,4)21(25)20(35-19(32)12-14-28(8)9)22(34-16(2)29)26(27,7)36-24;/h10,17,20-22,30,33H,1,11-15H2,2-9H3;1H/t17-,20-,21-,22-,24-,25-,26+,27-;/m0./s1

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C27H43NO8
Molecular Weight 509.6322
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including http://www.genome.jp/dbget-bin/www_bget?D01697 and https://www.ncbi.nlm.nih.gov/pubmed/12499623

Colforsin daropate (a derivative of Colforsin) is cardiotonic, adenylate cyclase activator. It is reported as an ingredient of Adehl in Japan. Colforsin daropate hydrochloride is used for the treatment of acute heart failure. Colforsin daropate is capable of directly stimulating adenylate cyclase, which in turn causes vasorelaxation via elevated intracellular concentrations of cyclic adenosine monophosphate, making it a useful therapeutic tool in treating cerebral vasospasm.

CNS Activity

CNS Penetrant
2554
Curator's Comment: COLFORSIN DAROPATE has been reported to penetrate the blood- brain barrier after peripheral administration and can thereby be used to activate adenylyl cyclase in the CNS

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Activator
1430
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
Adehl

Approved Use

Acute heart failure
PubMed

PubMed

TitleDatePubMed
Characterization of adenylyl cyclase isoforms in rat peripheral pulmonary arteries.
2001 Jun
Influence of colforsin daropate hydrochloride on internal mammary artery grafts.
2002 Apr
[Colforsin daropate does not affect the cerebral blood-flow in cardiac surgery patients under cardiopulmonary bypass].
2004 Apr
Effects of coleus forskohlii supplementation on body composition and hematological profiles in mildly overweight women.
2005 Dec 9
Chronic direct stimulation of adenylyl cyclase induces cardiac desensitization to catecholamine and beta-adrenergic receptor downregulation in rabbits.
2006 Nov
Beta-adrenoceptor-mediated vasodilation of retinal blood vessels is reduced in streptozotocin-induced diabetic rats.
2008 Aug-Sep
Colforsin-induced vasodilation in chronic hypoxic pulmonary hypertension in rats.
2010 Jun
Patents

Patents

US8865762
2
WO2011008052A3
2

Sample Use Guides

In Vivo Use Guide
0.75 ug kg-1 x min-1 colforsin daropate intravenously
Route of Administration: Intravenous
In Vitro Use Guide
COLFORSIN DAROPATE (10(-7)-10(-5) mol/l) inhibited [(3)H]thymidine incorporation into cultured rat MCs in a concentration-dependent manner.
Substance Class Chemical
Created
by admin
on Fri Dec 15 18:07:39 GMT 2023
Edited
by admin
on Fri Dec 15 18:07:39 GMT 2023
Record UNII
C6P4R272GT
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
COLFORSIN DAROPATE HYDROCHLORIDE
Common Name English
COLFORSIN DAROPATE HYDROCHLORIDE [JAN]
Common Name English
NKH-477
Code English
Colforsin dapropate hydrochloride [WHO-DD]
Common Name English
ADEHL
Brand Name English
.BETA.-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 (1:1)
Common Name English
6-(3-DIMETHYLAMINOPROPIONYL)FORSKOLIN HYDROCHLORIDE
Common Name English
Code System Code Type Description
EVMPD
SUB33262
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
SMS_ID
100000126205
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
CHEBI
31429
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
CAS
138605-00-2
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
EPA CompTox
DTXSID90930165
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
PUBCHEM
444028
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
FDA UNII
C6P4R272GT
Created by admin on Fri Dec 15 18:07:39 GMT 2023 , Edited by admin on Fri Dec 15 18:07:39 GMT 2023
PRIMARY
NIH
NCATS
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