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Details

Stereochemistry ABSOLUTE
Molecular Formula C27H43NO8
Molecular Weight 509.6322
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of COLFORSIN DAROPATE

SMILES

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

InChI

InChIKey=RSOZZQTUMVBTMR-XGUNBQNXSA-N
InChI=1S/C27H43NO8/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/t17-,20-,21-,22-,24-,25-,26+,27-/m0/s1

HIDE SMILES / InChI
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
2588
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
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Activator
1447
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
Adehl

Approved Use

Acute heart failure
PubMed

PubMed

TitleDatePubMed
Colforsin-induced vasodilation in chronic hypoxic pulmonary hypertension in rats.
2010-06
Beta-adrenoceptor-mediated vasodilation of retinal blood vessels is reduced in streptozotocin-induced diabetic rats.
2008-02-09
Chronic direct stimulation of adenylyl cyclase induces cardiac desensitization to catecholamine and beta-adrenergic receptor downregulation in rabbits.
2006-11
Effects of coleus forskohlii supplementation on body composition and hematological profiles in mildly overweight women.
2005-12-09
Functional changes in adenylyl cyclases and associated decreases in relaxation responses in mesenteric arteries from diabetic rats.
2005-11
Both milrinone and colforsin daropate attenuate the sustained pial arteriolar constriction seen after unclamping of an abdominal aortic cross-clamp in rabbits.
2005-07
Antiproliferative effects of NKH477, a forskolin derivative, on cytokine profile in rat lung allografts.
2005-04
Colforsin analogues: tritiation and characterization.
2004-12
Adenylyl cyclase type VI gene transfer reduces phospholamban expression in cardiac myocytes via activating transcription factor 3.
2004-09-10
Mechanism of cicaprost-induced desensitization in rat pulmonary artery smooth muscle cells involves a PKA-mediated inhibition of adenylyl cyclase.
2004-08
[Colforsin daropate does not affect the cerebral blood-flow in cardiac surgery patients under cardiopulmonary bypass].
2004-04
Effect of prophylactic bronchodilator treatment with intravenous colforsin daropate, a water-soluble forskolin derivative, on airway resistance after tracheal intubation.
2003-07
Expression of aquaporin 8 and its up-regulation by cyclic adenosine monophosphate in human WISH cells.
2003-04
Effect of mild hypothermia on inodilator-induced vasodilation of pial arterioles in cats.
2002-10
Role of cyclic nucleotides in ischemia and reperfusion injury of canine livers.
2002-04-15
Impaired intracellular signal transduction via cyclic AMP contributes to cerebral vasospasm in rats with subarachnoid hemorrhage.
2002-04
Influence of colforsin daropate hydrochloride on internal mammary artery grafts.
2002-04
Antiinflammatory effects of colforsin daropate hydrochloride, a novel water-soluble forskolin derivative.
2001-06
Characterization of adenylyl cyclase isoforms in rat peripheral pulmonary arteries.
2001-06
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 Mon Mar 31 21:24:22 GMT 2025
Edited
by admin
on Mon Mar 31 21:24:22 GMT 2025
Record UNII
1196KQZ976
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
COLFORSIN DAROPATE
Common 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
Preferred Name English
Code System Code Type Description
FDA UNII
1196KQZ976
Created by admin on Mon Mar 31 21:24:22 GMT 2025 , Edited by admin on Mon Mar 31 21:24:22 GMT 2025
PRIMARY
DRUG CENTRAL
729
Created by admin on Mon Mar 31 21:24:22 GMT 2025 , Edited by admin on Mon Mar 31 21:24:22 GMT 2025
PRIMARY
EPA CompTox
DTXSID20150415
Created by admin on Mon Mar 31 21:24:22 GMT 2025 , Edited by admin on Mon Mar 31 21:24:22 GMT 2025
PRIMARY
CAS
113462-26-3
Created by admin on Mon Mar 31 21:24:22 GMT 2025 , Edited by admin on Mon Mar 31 21:24:22 GMT 2025
PRIMARY
PUBCHEM
444029
Created by admin on Mon Mar 31 21:24:22 GMT 2025 , Edited by admin on Mon Mar 31 21:24:22 GMT 2025
PRIMARY
NIH
NCATS
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