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

Details

Stereochemistry ABSOLUTE
Molecular Formula C17H25N5O4
Molecular Weight 363.4115
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SDZ-WAG-994

SMILES

CO[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N2C=NC3=C2N=CN=C3NC4CCCCC4

InChI

InChIKey=JAKAFSGZUXCHLF-LSCFUAHRSA-N
InChI=1S/C17H25N5O4/c1-25-14-13(24)11(7-23)26-17(14)22-9-20-12-15(18-8-19-16(12)22)21-10-5-3-2-4-6-10/h8-11,13-14,17,23-24H,2-7H2,1H3,(H,18,19,21)/t11-,13-,14-,17-/m1/s1

HIDE SMILES / InChI

Description

SDZ-WAG-994 is a potent and selective A1 receptor agonist, discovered by Sandoz. SDZ-WAG-994 was able to induce a dose-related and sustained fall in blood pressure and heart rate in spontaneously hypertensive rats. The compound was investigated in patients with heart failure symptoms and moderate left ventricular systolic dysfunction, where it produced no effect. In patients with patients with permanent atrial fibrillation, SDZ-WAG-994 was able to limit the increase in mean heart rate during exercise. The compound was also tested for treatment of postoperative dental pain, but for all efficacy measures, SDZ-WAG-994 was not significantly different from placebo.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
23.0 nM [Kd]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Unknown
Primary
Unknown
Primary
Unknown

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
In a multicenter, double-blind, randomized, placebo-controlled, parallel group study, patients with permanent atrial fibrillation received 2 mg SDZWAG994 orally.
Route of Administration: Oral
In Vitro Use Guide
In vitro efficacy of SDZ-WAG-994 was measured by its ability to stimulate adenylate cyclase activity in rat adipocyte membranes. adipocytes from rat epididymal fat pads were homogenized, and adenylate cyclase activity was measured by the formation of [32P]cAMP from [32P]ATP. pEC50 for SDZ-WAG-994 was 6.4.