U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C14H13N3.ClH
Molecular Weight 259.734
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DEXFADROSTAT HYDROCHLORIDE

SMILES

Cl.N#CC1=CC=C(C=C1)[C@H]2CCCC3=CN=CN23

InChI

InChIKey=UKCVAQGKEOJTSR-PFEQFJNWSA-N
InChI=1S/C14H13N3.ClH/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14;/h4-7,9-10,14H,1-3H2;1H/t14-;/m1./s1

HIDE SMILES / InChI

Description

(+)-Fadrozole (FAD-286) is an aldosterone synthase inhibitor. The drug was tested in vivo in preclinical models of hypertension, heart failure and was shown to reduce retinal neovascularization in rats with oxygen-induced retinopathy.

Approval Year

Unknown
139,594

Targets

Primary TargetPharmacologyConditionPotency
Cytochrome P450 11B2, mitochondrial
3
Inhibitor
8,297
 3.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Congestive heart failure
54
 Primary
Preclinical
Unknown
Hypertension
567
 Primary
Preclinical
Unknown
Neovascular retinopathy
3
 Primary
Preclinical
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
In a preclinical study, (+)-fadrozole was given to rats at a dose of 30 mg/kg.
Route of Administration: Other
In Vitro Use Guide
(+)-Fadrozole inhibited angiotensin II-stimulated basal aldosterone production in NCI-H295R cells, showing a maximal effect at 10 nmol/l.
ACTIVE MOIETY
Structure of DEXFADROSTAT
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966