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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

Description

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.

Originator

Approval Year

Targets

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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as perpetrator​

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
rats: (0.01 to 0.30 mg/kg IV), (orally at 1, 3, 10, and 30 mg/kg)
Route of Administration: Other
In Vitro Use Guide
SAR407899 effectively inhibited THP-1 migration with an IC50 of 2.5 uM