DEXFADROSTAT

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C14H13N3
Molecular Weight	223.2731
Optical Activity	( + )
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

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

InChI

InChIKey=CLPFFLWZZBQMAO-CQSZACIVSA-N

InChI=1S/C14H13N3/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/t14-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C14H13N3
Molecular Weight	223.2731
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

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

Targets

Primary Target	Pharmacology	Condition	Potency
Cytochrome P450 11B2, mitochondrial 3	Inhibitor 8,297		3.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
Congestive heart failure 54	Primary	Preclinical	Unknown
Hypertension 567	Primary	Preclinical	Unknown
Neovascular retinopathy 3	Primary	Preclinical	Unknown

PubMed

PubMed

Title	Date	PubMed
No data available in table

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.

Substance Class	Chemical
Record UNII	IC1B8751F6
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

DEXFADROSTAT

Official Name

English

FADROZOLE, (R)-

Common Name

English

4-((5R)-5,6,7,8-TETRAHYDROIMIDAZO(1,5-A)PYRIDIN-5-YL)BENZONITRILE

Systematic Name

English

BENZONITRILE, 4-(5,6,7,8-TETRAHYDROIMIDAZO(1,5-A)PYRIDIN-5-YL)-, (R)-

Systematic Name

English

dexfadrostat [INN]

Common Name

English

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Code System

Code

Type

Description

CAS

102676-87-9

PRIMARY

FDA UNII

IC1B8751F6

PRIMARY

SMS_ID

300000042076

PRIMARY

INN

11875

PRIMARY

NCI_THESAURUS

C188586

PRIMARY

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Related Record

Type

Details


					H3988M64PU

FADROZOLE

RACEMATE -> ENANTIOMER

Amount:


					42REB33X4T

FADROZOLE PHOSPHATE, (R)-

SALT/SOLVATE -> PARENT

Amount:


					6T3TZF5EG8

DEXFADROSTAT HYDROCHLORIDE

SALT/SOLVATE -> PARENT

Amount:


					31I8UTYA8X

CYTOCHROME P450 11B2, MITOCHONDRIAL

TARGET -> INHIBITOR

Amount:

Showing 1 to 4 of 4 entries

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Type

Details


					IC1B8751F6

DEXFADROSTAT

ACTIVE MOIETY

Amount:

Showing 1 to 1 of 1 entries

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