GLOBALAGLIATIN

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H37N3O3S3
Molecular Weight	559.807
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=QIIVJLHCZUTGSD-CUBQBAPOSA-N

InChI=1S/C28H37N3O3S3/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)/t24-,28-/m0/s1

HIDE SMILES / InChI

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
Sources: http://www.selleckchem.com/products/ly2608204.html | http://adisinsight.springer.com/drugs/800033122
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

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glucokinase 4 Target ID: P35557 Gene ID: 2645.0 Gene Symbol: GCK Target Organism: Homo sapiens (Human) Sources: https://www.medkoo.com/products/8469 \| https://adisinsight.springer.com/drugs/800033122	Activator 1430		42.0 nM [EC50]
Hexokinase type IV 6 Target ID: CHEMBL3820 Sources: http://www.selleckchem.com/products/ly2608204.html	Activator 1430		42.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 259 Sources: http://adisinsight.springer.com/drugs/800033122	Primary		Phase I 428	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
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

Value	Dose	Analyte	Population
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

Title	Date	PubMed
Generation of stem cell-derived β-cells from patients with type 1 diabetes.	2016 May 10	27163171

Patents

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 05:50:55 GMT 2023` Edited by `admin` on `Sat Dec 16 05:50:55 GMT 2023`
Record UNII	5A0L003HEY
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GLOBALAGLIATIN

Common Name

English

SY-004

Code

English

(1R,2S)-2-CYCLOHEXYL-1-(4-(CYCLOPROPYLSULFONYL)PHENYL)-N-(5-((2-(1-PYRROLIDINYL)ETHYL)THIO)-2-THIAZOLYL)CYCLOPROPANECARBOXAMIDE

Systematic Name

English

LY-2608204

Common Name

English

Globalagliatin [WHO-DD]

Common Name

English

LY2608204

Code

English

Code System Code Type Description

FDA UNII

5A0L003HEY