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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

[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=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

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
Effect of mild hypothermia on inodilator-induced vasodilation of pial arterioles in cats.
2002 Oct
Expression of aquaporin 8 and its up-regulation by cyclic adenosine monophosphate in human WISH cells.
2003 Apr
Both milrinone and colforsin daropate attenuate the sustained pial arteriolar constriction seen after unclamping of an abdominal aortic cross-clamp in rabbits.
2005 Jul
Beta-adrenoceptor-mediated vasodilation of retinal blood vessels is reduced in streptozotocin-induced diabetic rats.
2008 Aug-Sep
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.
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
Common Name English
Code System Code Type Description
FDA UNII
1196KQZ976
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
DRUG CENTRAL
729
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
EPA CompTox
DTXSID20150415
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
CAS
113462-26-3
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
PUBCHEM
444029
Created by admin on Sat Dec 16 04:51:36 UTC 2023 , Edited by admin on Sat Dec 16 04:51:36 UTC 2023
PRIMARY
SUBSTANCE RECORD
Structure of COLFORSIN DAROPATE
NIH
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