| Cat. No. |
Product Name |
CAS No. |
Information |
| GY04379 |
GW 4064
|
278779-30-9 |
A potent and selective FXR agonist with EC50 of 15 nM in cell-free assay, >200-fold more potent than CDCA; has an EC50 of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors; significantly reducess serum alanine aminotransferase, aspartate aminotransferase, and lactate dehydrogenase, as well as other markers of liver damage in rat models of cholestasis. |
| GY07084 |
GSK-2324
|
1020567-30-9 |
GSK-2324 (GSK2324) is a potent, selective, full FXR agonist with EC50 of 120 nM in FRET assay; lowers body weight gain and serum glucose in a DIO mouse model of diabetes. |
| GY07083 |
LY-2562175
|
1103500-20-4 |
LY-2562175 (LY2562175, LY 2562175) is a novel potent, selective, partial FXR agonist with EC50 of 193 nM; does not promote transcriptional activation of other nuclear receptor, such as GR, PR, MR and AR (EC50>10 uM); lowers LDL and triglycerides while raising HDL in preclinical species. |
| GY02051 |
INT-767
|
1000403-03-1 |
INT-767 is a potent, selective, dual farnesoid X receptor (FXR) and TGR5 agonist with EC50 of 30 and 630 nM, respectively; fails to activate 15 other nuclear receptors involved in metabolic pathways, and does not inhibit cytochrome P450 enzymes; induces FXR-dependent lipid uptake by adipocytes and promotes TGR5-dependent glucagon-like peptide-1 (GLP-1) secretion by enteroendocrine cells; markedly decreases cholesterol and triglyceride levels in diabetic db/db mice. |
| GY04312 |
INT-747
|
459789-99-2 |
INT-747(Obeticholic acid, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective FXR agonist (EC50=99 nM); possesses anticholeretic activity in rat model of cholestasis. |
| GY04219 |
Fexaramine
|
574013-66-4 |
Fexaramine is a potent, specific FXR agonist with EC50 of 25 nM, more efficacious ligand for FXR than GW4064; shows no transcriptional activity against hRXRα, hPPARα/γ/δ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR; strongly induces target genes SHP, PLTP BSEP, and MRP-2 in the HEPG2 liver cell system; robustly induces FGF15, leading to alterations in BA composition. |
| GY04686 |
Tropifexor
|
1383816-29-2 |
Tropifexor (LJN-452, LJN452) is a novel highly potent, selective, orally acitive FXR full agonist with EC50 of 0.26 nM; shows no significant off-target activity (>10,000-fold selectivity for FXR) in a panel of targets, including TGR5 (>10 uM); demonstratesin vivo activity in rodent PD models, and shows potential for treatment of cholestatic liver diseases and NASH. |
| GY06418 |
MFA-1
|
139755-30-9 |
MFA-1 (Merck FXR agonist 1) is a potent, synthetic FXR agonist with EC50 of 16.9 nM in coactivator recruitment assays, displays 500-fold more potent than CDCA; displays an unexpected mode of binding and activation to FXR. |
| GY06417 |
Cilofexor
|
1418274-28-8 |
Cilofexor (GS-9674, GS9674, PX-104) is a novel specific, non-steroidal farnesoid X receptor (FXR) agonist that reduces liver fibrosis and ameliorates portal hypertension in rat NASH models. |
| GY06399 |
Nidufexor
|
1773489-72-7 |
Nidufexor (LMB763, LMB-763) is a novel potent farnesoid X receptor (FXR) agonist for the treatment of non-alcoholic steatohepatitis (NASH) and hepatobiliary disorders. |
$ USD
Select Your Country or Region
