ADOMEGLIVANT

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C32H36F3NO4
Molecular Weight	555.6277
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC(O[C@@H](CCC(F)(F)F)C2=CC=C(C=C2)C(=O)NCCC(O)=O)=CC(C)=C1C3=CC=C(C=C3)C(C)(C)C

InChI

InChIKey=FASLTMSUPQDLIB-MHZLTWQESA-N

InChI=1S/C32H36F3NO4/c1-20-18-26(19-21(2)29(20)23-10-12-25(13-11-23)31(3,4)5)40-27(14-16-32(33,34)35)22-6-8-24(9-7-22)30(39)36-17-15-28(37)38/h6-13,18-19,27H,14-17H2,1-5H3,(H,36,39)(H,37,38)/t27-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C32H36F3NO4
Molecular Weight	555.6277
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://en.pharmacodia.com/web/drug/1_22370.html | https://www.ncbi.nlm.nih.gov/pubmed/26681715 | https://www.ncbi.nlm.nih.gov/pubmed/28371155

Adomeglivant, also known as LY2409021, is a potent and selective glucagon receptor antagonist. Adomeglivant lowers blood glucose in healthy people and in those with type 2 diabetes. Blockade of glucagon signalling in patients with type 2 diabetes is well tolerated and results in substantial reduction of fasting and postprandial glucose with minimal hypoglycaemia, but with reversible increases in aminotransferases. Adomeglivant had been in phase II clinical trials by Eli Lilly for the treatment of type 2 diabetes mellitus. However, this research has been discontinued.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glucagon receptor 6 Target ID: CHEMBL1985 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25656305 \| https://professional.diabetes.org/abstract/glucose-lowering-efficacy-ly2409021-small-molecule-glucagon-receptor-antagonist-obob-mice	Antagonist 2849		6.66 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Type 2 diabetes mellitus 262 Sources: https://clinicaltrials.gov/ct2/show/NCT02091362 https://clinicaltrials.gov/ct2/show/NCT00871572	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1160 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3900 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15200 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
97900 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
333000 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1410000.01 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
58.6 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
56.8 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
57.9 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/25656305	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	ADOMEGLIVANT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P00AC7L	https://www.1pchem.com/search?query=1P00AC7L
AbovChem LLC	HY-19904
Chem Scene	CS-5729	http://www.chemscene.com/goproductList/searchProductList?productObj=CS-5729
Compound Cloud	91933867
eMolecules	275036906	https://orderbb.emolecules.com/search/#?query=275036906
eMolecules	303170678	https://orderbb.emolecules.com/search/#?query=303170678
eMolecules	89942146	https://orderbb.emolecules.com/search/#?query=89942146
mcule	MCULE-9754046865	https://mcule.com/MCULE-9754046865/
MedChem Express	HY-19904	https://www.medchemexpress.com/search.html?q=HY-19904&ft=&fa=&fp=
Molnova	M12058	https://www.molnova.com/en/serch-list.html?keywords=M12058
MolPort	MolPort-046-417-271	https://www.molport.com/shop/molecule-link/MolPort-046-417-271
MuseChem	I001829	https://www.musechem.com/product/I001829.html

PubMed

Title	Date	PubMed
Treatment with LY2409021, a glucagon receptor antagonist, increases liver fat in patients with type 2 diabetes.	2017-11	28371155
Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies.	2016-07	26681715

Patents

Sample Use Guides

In Vivo Use Guide

Type 2 Diabetes Mellitus: single daily dose of 20 milligrams (mg) Adomeglivant (LY2409021) administered orally in 1 of 2 treatment periods.

Route of Administration: Oral

In Vitro Use Guide

Adomeglivant (LY2409021) was identified as a potent and selective antagonist that inhibits the human glucagon receptor (hGCGR) with a Ki of 6.66 +/- 0.64 nM and the mouse GCGR with a Ki of 75.3 +/-11.4 nM.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:22:13 GMT 2025` Edited by `admin` on `Mon Mar 31 22:22:13 GMT 2025`
Record UNII	74Z5ZL2KVG
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ADOMEGLIVANT

Official Name

English

adomeglivant [INN]

Preferred Name

English

ADOMEGLIVANT, (-)-

Common Name

English

.BETA.-ALANINE, N-(4-((1S)-1-((4'-(1,1-DIMETHYLETHYL)-2,6-DIMETHYL(1,1'-BIPHENYL)-4-YL)OXY)-4,4,4-TRIFLUOROBUTYL)BENZOYL)-

Systematic Name

English

ADOMEGLIVANT [USAN]

Common Name

English

Adomeglivant [WHO-DD]

Common Name

English

3-(4-((1S)-1-((4'-TERT-BUTYL-2,6-DIMETHYLBIPHENYL-4-YL)OXY)-4,4,4- TRIFLUOROBUTYL)BENZAMIDO)PROPANOIC ACID

Systematic Name

English

LY-2409021

Code

English

LY2409021

Code

English

Code System Code Type Description

SMS_ID

100000174616