LY-377604

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C31H32N4O4
Molecular Weight	524.6102
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(CC1=CC=C(OC2=CC=C(C=N2)C(N)=O)C=C1)NC[C@H](O)COC3=CC=CC4=C3C5=C(N4)C=CC=C5

InChI

InChIKey=RBSGUQYXRDKPAE-QFIPXVFZSA-N

InChI=1S/C31H32N4O4/c1-31(2,16-20-10-13-23(14-11-20)39-28-15-12-21(17-33-28)30(32)37)34-18-22(36)19-38-27-9-5-8-26-29(27)24-6-3-4-7-25(24)35-26/h3-15,17,22,34-36H,16,18-19H2,1-2H3,(H2,32,37)/t22-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C31H32N4O4
Molecular Weight	524.6102
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900353 | https://adisinsight.springer.com/drugs/800013590

LY377604 is a human β3-adrenergic receptor agonist and β1- and β2-adrenergic receptor antagonist with no sympathomimetic activity at the β1- and β2-adrenergic receptors. Combination of LY377604 and a norepinephrine-serotonin uptake inhibitor (sibutramine) was studied in the treatment of obesity. LY377604 would ameliorate side effect of sibutramine treatment (increase in blood pressure and heart rate due to activation of the sympathetic nervous system).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Beta-3 adrenergic receptor 49 Target ID: P13945 Gene ID: 155.0 Gene Symbol: ADRB3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900353	Agonist 2678	2.4 nM [EC50]
Beta-1 adrenergic receptor 158 Target ID: P08588 Gene ID: 153.0 Gene Symbol: ADRB1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900353	Antagonist 2778	23.0 pM [Ki]
Beta-2 adrenergic receptor 203 Target ID: P07550\|\|\|Q53GA6\|\|\|Q9UCZ3 Gene ID: 154.0 Gene Symbol: ADRB2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900353	Antagonist 2778	12.0 pM [Ki]

PubMed

Title	Date	PubMed
Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.	2011 Aug 11	24900353

Substance Class	Chemical Created by `admin` on `Sat Dec 16 02:17:08 UTC 2023` Edited by `admin` on `Sat Dec 16 02:17:08 UTC 2023`
Record UNII	OCC6TB3P6K
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

LY-377604

Common Name

English

LY377604

Common Name

English

6-(4-(2-((3-(9H-CARBAZOL-4-YLOXY)-2-HYDROXYPROPYL)AMINO)-2-METHYLPROPYL)PHENOXY)-3-PYRIDINECARBOXAMIDE, S-

Common Name

English

Code System Code Type Description

CAS

204592-94-9