Search Result
Results for "
FXR agonist
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
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Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-153525
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- HY-151932
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FXR
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Inflammation/Immunology
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FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level .
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- HY-163466
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FXR
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Inflammation/Immunology
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FXR agonist 7 (compound 33) is a potent agonist of FXR, with EC50 of 0.1 nM. FXR agonist 7 shows high intestinal distribution, good anti-inflammatory activity .
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- HY-168331
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FXR
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Others
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FXR agonist 10 (Compound 27) is an agonist for FXR with an EC50 of 14.26 μM. FXR agonist 10 upregulates the expression of SHP and BSEP proteins, downregulates the expression of NTCP and CYP7A1 proteins. FXR agonist 10 ameliorates the ANIT-induced cholestasis in mouse model .
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- HY-164799
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FXR
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Inflammation/Immunology
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FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models .
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- HY-151959
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FXR
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD) .
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- HY-168332
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FXR
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Metabolic Disease
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FXR agonist 11 (Compound 14) is an FXR agonist with an EC50 of 1.2 μM and a maximum effect of 73.7%. FXR agonist 11 can significantly increase GSH levels in the liver and is used to study drug-induced liver injury diseases .
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- HY-168629
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FXR
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Metabolic Disease
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FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD and CCl4(HY-Y0298)-induced metabolic dysfunction-associated steatohepatitis mice .
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- HY-175516
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FXR
PPAR
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Inflammation/Immunology
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dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model .
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- HY-142159
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- HY-125996
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FXR
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Inflammation/Immunology
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NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease .
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- HY-50911
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FXR-450; XL335; WAY-362450
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FXR
Autophagy
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Metabolic Disease
Cancer
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Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM .
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- HY-50911R
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FXR
Autophagy
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Metabolic Disease
Cancer
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Turofexorate isopropyl (Standard) is the analytical standard of Turofexorate isopropyl. This product is intended for research and analytical applications. Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM .
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- HY-50108A
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- HY-50108
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- HY-N3209
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- HY-159845
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- HY-100443B
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- HY-100443A
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trans-PX-102
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FXR
Autophagy
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Metabolic Disease
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PX20606 trans racemate (PX-102 trans racemate) is a FXR agonist with EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively .
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- HY-103704
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- HY-160929
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- HY-N3891
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- HY-107418
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- HY-N15305
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FXR
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Inflammation/Immunology
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Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
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- HY-135400
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FXR
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Inflammation/Immunology
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Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-100443
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PX-102
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FXR
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Cancer
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PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy .
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- HY-135399
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FXR
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Inflammation/Immunology
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Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-135399A
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FXR
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Neurological Disease
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Tauro-obeticholic acid sodium is an active metabolite of Obeticholic acid (HY-12222). Obeticholic acid is a potent, selective and orally active FXR agonist.
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- HY-109096
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LMB763
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FXR
Autophagy
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Inflammation/Immunology
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Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH) .
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- HY-101273
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- HY-134988
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FXR
Phosphatase
Cytochrome P450
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Inflammation/Immunology
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EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
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- HY-169192
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FXR
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Inflammation/Immunology
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BAR-2227 (compound 3a) is a FXR agonist and LIFR inhibitor. BAR-2227 can be used to study liver fibrosis and inflammation .
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- HY-121110
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FXR
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Metabolic Disease
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Fexarene is a potent and selective nonsteroidal Farnesoid X Receptor (FXR) agonist with an EC50 of 36 nM. Fexarene can be used in studies of cholesterol and bile acid metabolism .
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- HY-12434
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- HY-169792
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FXR
Aminotransferases (Transaminases)
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Metabolic Disease
Inflammation/Immunology
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HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH) .
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- HY-B0172
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- HY-135400S
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FXR
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Inflammation/Immunology
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Glyco-obeticholic acid-d5 is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-117918
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- HY-135399S
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FXR
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Inflammation/Immunology
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Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid. Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
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- HY-139562
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FXR
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Metabolic Disease
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BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
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- HY-111049
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FXR
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Metabolic Disease
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GSK8062 is a farnesoid X receptor (FXR) agonist with activity that improves compound development parameters. Analog 1c of GSK8062 showed a reduction in weight gain and serum glucose levels .
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- HY-12222
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INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid
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FXR
Autophagy
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Others
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Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-147296
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MET642
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FXR
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Inflammation/Immunology
Cancer
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Omesdafexor (MET642) is an oral FXR agonist. Omesdafexor can improve colitis induced by adoptive T cell transfer,promote intestinal antimicrobial function, barrier function and inhibit inflammation .
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- HY-109197
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EYP001
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FXR
HBV
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Infection
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Vonafexor (EYP001) is an orally active, non-steroidal and selective FXR agonist. Vonafexor shows significant HBsAg reduction when combined with Peg-IFNα. Vonafexor can be used for anti-HBV research .
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- HY-W653920
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Isotope-Labeled Compounds
FXR
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Inflammation/Immunology
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Tauro 6-ethlchenodeoxycholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-10912
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FXR
Autophagy
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Others
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Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .
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- HY-N4063
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FXR
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Inflammation/Immunology
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Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation .
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- HY-N10640
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FXR
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Inflammation/Immunology
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Alismanol M is a farnesoid X receptor (FXR) agonist with an EC50 value of 50.25 μM. Alismanol M is a protostane-type triterpenoid that can be isolated from the rhizome of Alisma orientale. Alismanol M can be used for the research of cholestasis and nonalcoholic steatohepatitis .
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- HY-109083
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GS-9674
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FXR
Autophagy
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Inflammation/Immunology
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Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research .
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- HY-B0172R
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3α-Hydroxy-5β-cholanic acid (Standard)
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Reference Standards
Autophagy
Endogenous Metabolite
Apoptosis
FXR
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Metabolic Disease
Cancer
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Lithocholic acid (Standard) is the analytical standard of Lithocholic acid. This product is intended for research and analytical applications. Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist .
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- HY-12222S1
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FXR
Autophagy
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Others
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Obeticholic Acid-d4 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-W587451
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OCA-3-glucuronide disodium
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FXR
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Metabolic Disease
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Cholic acid 3-O-glucuronide (OCA-3-glucuronide) disodium is a farnesoid X receptor (FXR) agonist with an EC50 value of 91.5 μM. Cholic acid 3-O-glucuronide is promising for research of bile acid metabolism and detoxification .
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- HY-113567
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FXR
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Metabolic Disease
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GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively .
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- HY-12222S
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INT-747-d5; 6-ECDCA-d5; 6-Ethylchenodeoxycholic acid-d5
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FXR
Autophagy
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Others
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Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-12222R
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INT-747 (Standard); 6-ECDCA (Standard); 6-Ethylchenodeoxycholic acid (Standard)
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Reference Standards
FXR
Autophagy
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Others
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Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-A0248BR
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Reference Standards
Antibiotic
Bacterial
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Infection
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Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-10626
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LXR
FXR
ROR
Apoptosis
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Cardiovascular Disease
Metabolic Disease
Cancer
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T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
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- HY-168327
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FXR
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Inflammation/Immunology
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LH10 is a fexaramine-based agonist for FXR with an EC50 of 0.14 μM. LH10 exhibits liver protection efficacy, ameliorates the alpha naphthylisothiocyanate (ANIT)-induced cholestasis, APAP (HY-66005)-induced acute liver injury and non-alcoholic steatohepatitis (NASH) in mouse models .
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- HY-150787
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FXR
Cytochrome P450
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Metabolic Disease
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BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis .
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- HY-10912R
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FXR
Autophagy
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Others
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Fexaramine (Standard) is the analytical standard of Fexaramine. This product is intended for research and analytical applications. Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors .
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- HY-139418
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FXR
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Cancer
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PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models .
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- HY-10626R
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Reference Standards
LXR
FXR
ROR
Apoptosis
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Cardiovascular Disease
Metabolic Disease
Cancer
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T0901317 (Standard) is the analytical standard of T0901317. This product is intended for research and analytical applications. T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
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- HY-N4294
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FXR
Insecticide
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Infection
Metabolic Disease
Inflammation/Immunology
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Arjungenin, a pentacyclic triterpenoid compound, is a FXR agonist. Arjungenin can improve insulin sensitivity by regulating the function of fat cells. Arjungenin exhibits moderate free radical scavenging activity. Arjungenin has growth inhibitory activity against the insect Spilarctia obliqua. Arjungenin has significant antiviral activity against a series of viruses such as chikungunya Virus (CHIKV) .
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- HY-168713
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FXR
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Metabolic Disease
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LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
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- HY-153114
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FXR
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Inflammation/Immunology
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HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
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- HY-N4294R
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Reference Standards
FXR
Insecticide
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Infection
Metabolic Disease
Inflammation/Immunology
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Arjungenin (Standard) is the analytical standard of Arjungenin. This product is intended for research and analytical applications. Arjungenin, a pentacyclic triterpenoid compound, is a FXR agonist. Arjungenin can improve insulin sensitivity by regulating the function of fat cells. Arjungenin exhibits moderate free radical scavenging activity. Arjungenin has growth inhibitory activity against the insect Spilarctia obliqua. Arjungenin has significant antiviral activity against a series of viruses such as chikungunya Virus (CHIKV).
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- HY-177050
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G protein-coupled Bile Acid Receptor 1
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Metabolic Disease
Inflammation/Immunology
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RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly outperforming Betulinic acid (HY-10529) (EC50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS (HY-D1056)-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes [1][2][3][4][5].
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- HY-N3431
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AMPK
PD-1/PD-L1
FXR
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
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Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure .
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- HY-N0910
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PI3K
mTOR
Akt
Apoptosis
p38 MAPK
ERK
Transmembrane Glycoprotein
Glutathione Reductase (GR)
Estrogen Receptor/ERR
Calcium Channel
Ferroptosis
G protein-coupled Bile Acid Receptor 1
FXR
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Cardiovascular Disease
Metabolic Disease
Cancer
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NotoginsenosideFt1 is a saponin found in Panax notoginseng. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8 + T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca 2+ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y12 receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance .
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Product Name |
Target |
Research Area |
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- HY-A0248BR
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Reference Standards
Antibiotic
Bacterial
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Infection
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Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W653920
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Tauro 6-ethlchenodeoxycholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist .
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- HY-12222S1
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Obeticholic Acid-d4 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-12222S
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Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy .
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- HY-135400S
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Glyco-obeticholic acid-d5 is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist .
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- HY-135399S
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Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid. Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
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