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

Details

Stereochemistry ABSOLUTE
Molecular Formula C10H18N2OS
Molecular Weight 214.328
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of NGX-267

SMILES

CC[C@@H]1SC2(CCN(C)CC2)NC1=O

InChI

InChIKey=PHOZOHFUXHPOCK-QMMMGPOBSA-N
InChI=1S/C10H18N2OS/c1-3-8-9(13)11-10(14-8)4-6-12(2)7-5-10/h8H,3-7H2,1-2H3,(H,11,13)/t8-/m0/s1

HIDE SMILES / InChI

Molecular Formula C10H18N2OS
Molecular Weight 214.328
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

NGX267 is a partial muscarinic receptor agonist with functionally specific M1 and M3 receptor activity, developed by Torrey Pines Therapeutics(TPTX) for the treatment of Xerostomia, Alzheimer’s disease and cognitive deficits in schizophrenia. NGX-267 had been in phase II clinical trials for the treatment of Xerostomia, however, all researchers on this drug candidate were discontinued.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
30.0 nM [EC50]
1.57 µM [EC50]
1.56 µM [EC50]
44.0 nM [EC50]
0.85 µM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown

PubMed

Sample Use Guides

In Vivo Use Guide
1 -35 mg as single oral dose
Route of Administration: Oral
In Vitro Use Guide
PC12 cells stably transfected with M1 mAChR were used for activity evaluation. Cells were treated with NGX267(50ng/mL). NGX267 inhibit Abeta- and oxidative-stress-induced cell death and apoptosis in PC12 cells transfected with the M1 muscarinic receptor.
Substance Class Chemical
Record UNII
8D3PZX7G73
Record Status Validated (UNII)
Record Version