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)
| Molecular Formula | C24H29NO2 |
| Molecular Weight | 363.4926 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/7636877Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/10951538 |
https://www.ncbi.nlm.nih.gov/pubmed/12374698 |
https://www.ncbi.nlm.nih.gov/pubmed/18483313
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7636877
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/10951538 |
https://www.ncbi.nlm.nih.gov/pubmed/12374698 |
https://www.ncbi.nlm.nih.gov/pubmed/18483313
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 |
|---|---|---|---|
Target ID: CHEMBL2363070 Sources: https://www.ncbi.nlm.nih.gov/pubmed/7636877 |
3.0 nM [Kd] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Tributyltin engages multiple nuclear receptor pathways and suppresses osteogenesis in bone marrow multipotent stromal cells. | 2015-06-15 |
|
| Mechanisms of action of hormone-sensitive lipase in mouse Leydig cells: its role in the regulation of the steroidogenic acute regulatory protein. | 2013-03-22 |
|
| Tributyltin synergizes with 20-hydroxyecdysone to produce endocrine toxicity. | 2011-09 |
|
| In silico prediction of pregnane X receptor activators by machine learning approaches. | 2007-01 |
|
| Identification of biomarkers modulated by the rexinoid LGD1069 (bexarotene) in human breast cells using oligonucleotide arrays. | 2006-12-15 |
|
| Neu-induced retroviral rat mammary carcinogenesis: a novel chemoprevention model for both hormonally responsive and nonresponsive mammary carcinomas. | 2006-07-01 |
|
| PPARalpha activators and fasting induce the expression of adipose differentiation-related protein in liver. | 2006-05 |
|
| Organotin compounds enhance 17beta-hydroxysteroid dehydrogenase type I activity in human choriocarcinoma JAr cells: potential promotion of 17beta-estradiol biosynthesis in human placenta. | 2006-04-28 |
|
| Receptor-selective retinoids inhibit the growth of normal and malignant breast cells by inducing G1 cell cycle blockade. | 2006-03 |
|
| Coactivation of liver receptor homologue-1 by peroxisome proliferator-activated receptor gamma coactivator-1alpha on aromatase promoter II and its inhibition by activated retinoid X receptor suggest a novel target for breast-specific antiestrogen therapy. | 2005-12-15 |
|
| Trialkyltin compounds bind retinoid X receptor to alter human placental endocrine functions. | 2005-10 |
|
| Thiazolidinediones inhibit proliferation of microvascular and macrovascular cells by a PPARgamma-independent mechanism. | 2005-03 |
|
| Molecular cloning and characterization of two novel human RXR alpha splice variants. | 2004-09 |
|
| Retinoid X receptor (RXR) agonist-induced antagonism of farnesoid X receptor (FXR) activity due to absence of coactivator recruitment and decreased DNA binding. | 2003-03-21 |
|
| Prevention and treatment of experimental breast cancer with the combination of a new selective estrogen receptor modulator, arzoxifene, and a new rexinoid, LG 100268. | 2002-10 |
|
| The effects of rexinoids and rosiglitazone on body weight and uncoupling protein isoform expression in the Zucker fa/fa rat. | 2000-12 |
|
| Insulin sensitizer, troglitazone, directly inhibits aromatase activity in human ovarian granulosa cells. | 2000-05-19 |
|
| Therapeutic applications for ligands of retinoid receptors. | 2000-01 |
|
| The pregnane X receptor: a promiscuous xenobiotic receptor that has diverged during evolution. | 2000-01 |
|
| Growth inhibition of myeloid leukemia cells by troglitazone, a ligand for peroxisome proliferator activated receptor gamma, and retinoids. | 1999-11 |
|
| Activation of specific RXR heterodimers by an antagonist of RXR homodimers. | 1996-10-03 |
|
| Synthesis of high specific activity [3H]-9-cis-retinoic acid and its application for identifying retinoids with unusual binding properties. | 1994-02-04 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10951538
In obesity studies LG100268 was dosed orally once daily at 20 mg/kg to Zucker rats.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7636877
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 19:10:04 GMT 2025
by
admin
on
Mon Mar 31 19:10:04 GMT 2025
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UVU4X1103P
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Validated (UNII)
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