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

Details

Stereochemistry ABSOLUTE
Molecular Formula C10H15NO.C4H4O4
Molecular Weight 281.3044
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of TALSACLIDINE FUMARATE

SMILES

OC(=O)\C=C\C(O)=O.C#CCO[C@H]1CN2CCC1CC2

InChI

InChIKey=SBCXBWBXWKVIFK-PBBCPHEYSA-N
InChI=1S/C10H15NO.C4H4O4/c1-2-7-12-10-8-11-5-3-9(10)4-6-11;5-3(6)1-2-4(7)8/h1,9-10H,3-8H2;1-2H,(H,5,6)(H,7,8)/b;2-1+/t10-;/m0./s1

HIDE SMILES / InChI

Molecular Formula C4H4O4
Molecular Weight 116.0722
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Molecular Formula C10H15NO
Molecular Weight 165.2322
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
18.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.7 ng/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TALSACLIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
730 ng/mL
160 mg single, oral
dose: 160 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TALSACLIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
12 ng × h/mL
0.5 mg single, oral
dose: 0.5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TALSACLIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4500 ng × h/mL
160 mg single, oral
dose: 160 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
TALSACLIDINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
99%
TALSACLIDINE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

Talsaclidine is administered orally at a dose of 24 mg, three times a day.
Route of Administration: Oral
In Vitro Use Guide
Isolated tracheal muscle from guinea-pigs was incubated with 1-3000 uM of talsaclidine to test the muscarinic receptor agonism.
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:47:58 GMT 2023
Edited
by admin
on Fri Dec 15 15:47:58 GMT 2023
Record UNII
6A7C8SIH42
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TALSACLIDINE FUMARATE
USAN   WHO-DD  
USAN  
Official Name English
WAL 2014 FU
Code English
Talsaclidine fumarate [WHO-DD]
Common Name English
TALSACLIDINE FUMARATE [USAN]
Common Name English
WAL-2014-FU
Code English
WAL-2014FU
Code English
Classification Tree Code System Code
NCI_THESAURUS C47796
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL2111051
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
MESH
C079885
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
NCI_THESAURUS
C152500
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
PUBCHEM
6918244
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
CAS
147025-54-5
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
FDA UNII
6A7C8SIH42
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
USAN
GG-45
Created by admin on Fri Dec 15 15:47:58 GMT 2023 , Edited by admin on Fri Dec 15 15:47:58 GMT 2023
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY