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

Details

Stereochemistry ABSOLUTE
Molecular Formula C29H37N5O2
Molecular Weight 487.6364
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GSK-3008348 FREE BASE

SMILES

CC1=NN(C(C)=C1)C2=CC=CC(=C2)[C@@H](CN3CC[C@@H](CCC4=CC=C5CCCN=C5N4)C3)CC(O)=O

InChI

InChIKey=ZMXBIIQMSGOIRZ-RCZVLFRGSA-N
InChI=1S/C29H37N5O2/c1-20-15-21(2)34(32-20)27-7-3-5-24(16-27)25(17-28(35)36)19-33-14-12-22(18-33)8-10-26-11-9-23-6-4-13-30-29(23)31-26/h3,5,7,9,11,15-16,22,25H,4,6,8,10,12-14,17-19H2,1-2H3,(H,30,31)(H,35,36)/t22-,25-/m1/s1

HIDE SMILES / InChI
Molecular Formula C29H37N5O2
Molecular Weight 487.6364
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
102 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
30 μg single, respiratory
dose: 30 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
501 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1922 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7243 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29393 pg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
285 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
30 μg single, respiratory
dose: 30 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1765 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6850 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
29093 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
82205 pg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
10.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
100 μg single, respiratory
dose: 100 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
300 μg single, respiratory
dose: 300 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
8.97 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
1000 μg single, respiratory
dose: 1000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
7.95 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/29532104/
3000 μg single, respiratory
dose: 3000 μg
route of administration: Respiratory
experiment type: SINGLE
co-administered:
GSK-3008348 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
Safety, tolerability and pharmacokinetics of GSK3008348, a novel integrin αvβ6 inhibitor, in healthy participants.
2018-06
Substance Class Chemical
Created
by admin
on Wed Apr 02 19:47:31 GMT 2025
Edited
by admin
on Wed Apr 02 19:47:31 GMT 2025
Record UNII
L6EE7H64YF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GSK3008348 FREE BASE
Preferred Name English
GSK-3008348 FREE BASE
Common Name English
(?S,3R)-?-[3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-1-pyrrolidinebutanoic acid
Systematic Name English
1-Pyrrolidinebutanoic acid, ?-[3-(3,5-dimethyl-1H-pyrazol-1-yl)phenyl]-3-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl]-, (?S,3R)-
Systematic Name English
Code System Code Type Description
FDA UNII
L6EE7H64YF
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
PUBCHEM
86272865
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
CAS
1629249-33-7
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
SMS_ID
300000042457
Created by admin on Wed Apr 02 19:47:31 GMT 2025 , Edited by admin on Wed Apr 02 19:47:31 GMT 2025
PRIMARY
Related Record Type Details
HUMAN TRANSFORMING GROWTH FACTOR .BETA.-1
INHIBITION OF ACTIVATION->TARGE
Inhibited Smad2 phosphorylation in a concentration-dependent manner
EC50
Structure of GSK-3008348
SALT/SOLVATE -> PARENT
INTEGRIN ALPHA-V/BETA-6
TARGET->DEGRADER
induced ?v?6 internalization and degradation. ligand-induced ?v?6 integrin internalization following 2?h incubation with NHBE cells.
EC50
Related Record Type Details
Structure of GSK-3008348 FREE BASE
ACTIVE MOIETY
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966