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Details

Stereochemistry ACHIRAL
Molecular Formula C14H16N2O2
Molecular Weight 244.289
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SAR-407899

SMILES

O=C1NC=CC2=C1C=CC(OC3CCNCC3)=C2

InChI

InChIKey=IPEXHQGMTHOKQV-UHFFFAOYSA-N
InChI=1S/C14H16N2O2/c17-14-13-2-1-12(9-10(13)3-8-16-14)18-11-4-6-15-7-5-11/h1-3,8-9,11,15H,4-7H2,(H,16,17)

HIDE SMILES / InChI

Molecular Formula C14H16N2O2
Molecular Weight 244.289
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

SAR407899 is a potent, ATP-competitive Rho kinase inhibitor. It antihypertensive action in animals. Sanofi is developing SAR 407899 for the treatment of microvascular angina (Syndrome X). It was previously being developed in clinical trials for the treatment of diabetic neuropathies, diabetic nephropathies, erectile dysfunction, pulmonary hypertension, hypertension and kidney disorders, but development was discontinued for those indications.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
36.0 nM [Ki]
276.0 nM [IC50]
Conditions
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG



OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Pharmacological characterization of SAR407899, a novel rho-kinase inhibitor.
2009 Sep
Erectile properties of the Rho-kinase inhibitor SAR407899 in diabetic animals and human isolated corpora cavernosa.
2012 Mar 23
The Rho kinase inhibitor SAR407899 potently inhibits endothelin-1-induced constriction of renal resistance arteries.
2012 May
Activation of Rac-1 and RhoA contributes to podocyte injury in chronic kidney disease.
2013
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment: SAR407899 is in clinical trials but dosage and regimen are unknown. http://adisinsight.springer.com/drugs/800026023
rats: (0.01 to 0.30 mg/kg IV), (orally at 1, 3, 10, and 30 mg/kg)
Route of Administration: Other
SAR407899 effectively inhibited THP-1 migration with an IC50 of 2.5 uM
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:33:21 GMT 2023
Edited
by admin
on Sat Dec 16 08:33:21 GMT 2023
Record UNII
3B974D670O
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SAR-407899
Code English
1(2H)-ISOQUINOLINONE, 6-(4-PIPERIDINYLOXY)-
Systematic Name English
SAR407899
Code English
6-(4-PIPERIDINYLOXY)-1(2H)-ISOQUINOLINONE
Systematic Name English
Code System Code Type Description
ChEMBL
CHEMBL1667969
Created by admin on Sat Dec 16 08:33:21 GMT 2023 , Edited by admin on Sat Dec 16 08:33:21 GMT 2023
PRIMARY
FDA UNII
3B974D670O
Created by admin on Sat Dec 16 08:33:21 GMT 2023 , Edited by admin on Sat Dec 16 08:33:21 GMT 2023
PRIMARY
CAS
923359-38-0
Created by admin on Sat Dec 16 08:33:21 GMT 2023 , Edited by admin on Sat Dec 16 08:33:21 GMT 2023
PRIMARY
SMS_ID
300000042524
Created by admin on Sat Dec 16 08:33:21 GMT 2023 , Edited by admin on Sat Dec 16 08:33:21 GMT 2023
PRIMARY
PUBCHEM
15604510
Created by admin on Sat Dec 16 08:33:21 GMT 2023 , Edited by admin on Sat Dec 16 08:33:21 GMT 2023
PRIMARY
Related Record Type Details
SALT/SOLVATE -> PARENT
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY