LG 100268

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H29NO2
Molecular Weight	363.4926
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1=C(C=C2C(=C1)C(C)(C)CCC2(C)C)C3(CC3)C4=CC=C(C=N4)C(O)=O

InChI

InChIKey=SLXTWXQUEZSSTJ-UHFFFAOYSA-N

InChI=1S/C24H29NO2/c1-15-12-18-19(23(4,5)9-8-22(18,2)3)13-17(15)24(10-11-24)20-7-6-16(14-25-20)21(26)27/h6-7,12-14H,8-11H2,1-5H3,(H,26,27)

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Description

LG 100268 (LGD 1268) is retionid X receptor agonist, originated in Ligand Pharmaceuticals. LG 100268 demonstrated efficacy in preclinical models of obesity, breast and lung cancer.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Retinoid X receptor 4	Agonist 2,752		3.0 nM [Kd]

Conditions

Condition	Modality	Highest Phase	Product
Obesity 206	Primary	Preclinical	Unknown
Breast cancer 432	Primary	Preclinical	Unknown
Lung cancer 70	Primary	Preclinical	Unknown

PubMed

Show entries

Title	Date	PubMed
Activation of specific RXR heterodimers by an antagonist of RXR homodimers.	1996 Oct 3	8837780
The effects of rexinoids and rosiglitazone on body weight and uncoupling protein isoform expression in the Zucker fa/fa rat.	2000 Dec	11145125
Therapeutic applications for ligands of retinoid receptors.	2000 Jan	10637371
The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution.	2000 Jan	10628745
Insulin sensitizer, troglitazone, directly inhibits aromatase activity in human ovarian granulosa cells.	2000 May 19	10814527

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Patents

Sample Use Guides

In Vivo Use Guide

In obesity studies LG100268 was dosed orally once daily at 20 mg/kg to Zucker rats.

Route of Administration: Oral

In Vitro Use Guide

Receptor binding assays for RXRs were performed using [3H]-9-cis-RA as the radioligand for RXRs. EC50 values we determined by contransfection assay performed with CV-1 cells.

Show entries

Name

Type

Language

LG 100268

Common Name

English

AGN 192620

Preferred Name

English

LG-268

Code

English

AGN-192620

Code

English

6-(1-(3,5,5,8,8-PENTAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)CYCLOPROPYL)NICOTINIC ACID

Systematic Name

English

Showing 1 to 5 of 19 entries

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Code System

Code

Type

Description

FDA UNII

UVU4X1103P

PRIMARY

MESH

C095104

PRIMARY

EPA CompTox

DTXSID90165354

PRIMARY

CAS

153559-76-3

PRIMARY

PUBCHEM

3922

PRIMARY

Showing 1 to 5 of 6 entries

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SUBSTANCE RECORD


					UVU4X1103P

LG 100268