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Details

Stereochemistry ABSOLUTE
Molecular Formula C14H13N3.H3O4P
Molecular Weight 321.2683
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FADROZOLE PHOSPHATE, (R)-

SMILES

OP(O)(O)=O.[H][C@@]1(CCCC2=CN=CN12)C3=CC=C(C=C3)C#N

InChI

InChIKey=QPMXWEHWAGTWOC-PFEQFJNWSA-N
InChI=1S/C14H13N3.H3O4P/c15-8-11-4-6-12(7-5-11)14-3-1-2-13-9-16-10-17(13)14;1-5(2,3)4/h4-7,9-10,14H,1-3H2;(H3,1,2,3,4)/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
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