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Details

Stereochemistry ABSOLUTE
Molecular Formula C28H37N3O3S3.ClH
Molecular Weight 596.268
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GLOBALAGLIATIN HYDROCHLORIDE

SMILES

Cl.O=C(NC1=NC=C(SCCN2CCCC2)S1)[C@@]3(C[C@H]3C4CCCCC4)C5=CC=C(C=C5)S(=O)(=O)C6CC6

InChI

InChIKey=FRUQQNDJVRDIRH-JOFLZTHPSA-N
InChI=1S/C28H37N3O3S3.ClH/c32-26(30-27-29-19-25(36-27)35-17-16-31-14-4-5-15-31)28(18-24(28)20-6-2-1-3-7-20)21-8-10-22(11-9-21)37(33,34)23-12-13-23;/h8-11,19-20,23-24H,1-7,12-18H2,(H,29,30,32);1H/t24-,28-;/m0./s1

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C28H37N3O3S3
Molecular Weight 559.807
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27163171

LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM. Eli Lilly is developing LY 2608204 as an orally administered, once-daily therapy for type 2 diabetes. LY-2608204 is in phase I clinical trials for the treatment of type 2 diabetes.

Originator

Eli Lilly
237
Curator's Comment: # Eli Lilly

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Glucokinase
4
Target ID: P35557
Gene ID: 2645.0
Gene Symbol: GCK
Target Organism: Homo sapiens (Human)
Activator
1430
 42.0 nM [EC50]
Activator
1430
 42.0 nM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase I
428
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
29.36 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
69.43 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
80 mg 1 times / day steady-state, oral
dose: 80 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
183.88 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
160 mg 1 times / day steady-state, oral
dose: 160 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
342 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
471.5 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
320 mg 1 times / day steady-state, oral
dose: 320 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
369.71 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1009.35 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
80 mg 1 times / day steady-state, oral
dose: 80 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3036.75 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
160 mg 1 times / day steady-state, oral
dose: 160 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
6028.2 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
240 mg 1 times / day steady-state, oral
dose: 240 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
9218.38 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/33125674/
320 mg 1 times / day steady-state, oral
dose: 320 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LY-2608204 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
PubMed

PubMed

TitleDatePubMed
Generation of stem cell-derived β-cells from patients with type 1 diabetes.
2016 May 10
Patents

Patents

20100160395
2
8063079
2
US8063079
2
WO2010080333A1
2

Sample Use Guides

In Vivo Use Guide
Oral capsules of LY2608204 given once daily at a starting dose of 160mg, which may be titrated in 3 dose escalations to 240mg, 320mg and 400mg, with a 7-day treatment duration at each dose level for up to 28 days total treatment.
Route of Administration: Oral
In Vitro Use Guide
Treatment with 1uM of LY2608204 increases insulin release in T1D and ND SC-β cell lines at both low- and high-glucose challenges compared with control by a factor of 2.0 on average.
Substance Class Chemical
Created
by admin
on Sat Dec 16 18:08:02 GMT 2023
Edited
by admin
on Sat Dec 16 18:08:02 GMT 2023
Record UNII
CH9BD8J28R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GLOBALAGLIATIN HYDROCHLORIDE
Common Name English
SY-004 HYDROCHLORIDE
Code English
2-CYCLOHEXYL-1-(4-(CYCLOPROPYLSULFONYL)PHENYL)-N-(5-((2-(1-PYRROLIDINYL)ETHYL)THIO)-2-THIAZOLYL)-, HYDROCHLORIDE (1:1), (1R,2S)-
Systematic Name English
LY2608204 HYDROCHLORIDE
Code English
LY-2608204 HYDROCHLORIDE
Code English
Globalagliatin hydrochloride [WHO-DD]
Common Name English
Code System Code Type Description
PUBCHEM
162623518
Created by admin on Sat Dec 16 18:08:03 GMT 2023 , Edited by admin on Sat Dec 16 18:08:03 GMT 2023
PRIMARY
FDA UNII
CH9BD8J28R
Created by admin on Sat Dec 16 18:08:03 GMT 2023 , Edited by admin on Sat Dec 16 18:08:03 GMT 2023
PRIMARY
Related Record Type Details
Structure of GLOBALAGLIATIN
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of GLOBALAGLIATIN
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