FXR-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/FXR.html FXRFXR; NR1H4Farnesoid X receptor (FXR) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. FXR regulatesthe expression of various genes by binding to DNA either as a monomer or a heterodimer with the common partne

2、r for NRs,retinoid x receptor (RXR), to FXR response elements. Two known FXR genes exist, the FXR and FXR.FXR is mainly expressed in liver and small intestine, where it plays an important role in bile acid, lipid, and glucose metabolism. FXRaffects several metabolic pathways through its specific tar

3、get genes, regulating bile acid (BA) synthesis and homeostasis, glucoseand lipid metabolism, also exhibiting a crucial role in intestinal bacterial growth and liver regeneration.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/FXR.html FXR HYPERLINK https:/www.MedChemE/Targets/FXR.html HYPERLINK

4、 https:/www.MedChemE/Targets/FXR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/FXR.html HYPERLINK https:/www.MedChemE/Targets/FXR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/FXR.html HYPERLINK https:/www.MedChemE/Targets/FXR.html Antagonists HYPERLINK https:/www.MedChemE/Targets/FX

5、R.html HYPERLINK https:/www.MedChemE/Targets/FXR.html & HYPERLINK https:/www.MedChemE/Targets/FXR.html HYPERLINK https:/www.MedChemE/Targets/FXR.html Activators HYPERLINK https:/www.MedChemE/_-_-PX20606_trans_isomer.html (-)-PX20606 HYPERLINK https:/www.MedChemE/_-_-PX20606_trans_isomer.html HYPERLI

6、NK https:/www.MedChemE/_-_-PX20606_trans_isomer.html trans HYPERLINK https:/www.MedChemE/_-_-PX20606_trans_isomer.html HYPERLINK https:/www.MedChemE/_-_-PX20606_trans_isomer.html isomer(-)-PX-102 trans isomer; (-)-PX-104) Cat. No.: HY-100443B HYPERLINK https:/www.MedChemE/BAR502.html BAR502Cat. No.:

7、 HY-101273(-)-PX20606 trans isomer is a FXR agonist withEC s of 18 and 29 nM for FXR in FRET and M1H50assay, respectively.BAR502 is a dual FXR and GPBAR1 agonist withIC values of 2 M and 0.4 M, respectively.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 2 mgPurity: 98.0%Clinical Data

8、: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-986318.html BMS-986318Cat. No.: HY-139562 HYPERLINK https:/www.MedChemE/Chenodeoxycholic-Acid.html Chenodeoxycholic HYPERLINK https:/www.MedChemE/Chenodeoxycholic-Acid.html HYPERLINK https:/

9、www.MedChemE/Chenodeoxycholic-Acid.html Acid(CDCA) Cat. No.: HY-76847BMS-986318 is a potent nonbile acid FXR agonistwith EC s of 53 and 350 nM in the FXR Gal4 and50SRC-1 recruitment assays, respectively. BMS-986318has a suitable ADME profile, and demonstratesefficacy in the mouse bile duct ligation

10、model ofliver cholestasis and fibrosis.Chenodeoxycholic Acid is a hydrophobic primarybile acid that activates nuclear receptors (FXR)involved in cholesterol metabolism.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 m

11、g HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-13c.html Chenodeoxycholic HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-13c.html HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-13c.html acid-13C(CDCA-13C) Cat. No.: HY-76847S2 HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d4.htm

12、l Chenodeoxycholic HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d4.html HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d4.html Acid-d4(CDCA-d4) Cat. No.: HY-76847SChenodeoxycholic acid-13C (CDCA-13C) is the13C-labeled Chenodeoxycholic Acid.Chenodeoxycholic Acid is a hydrophobic primarybi

13、le acid that activates nuclear receptors (FXR)involved in cholesterol metabolism.Chenodeoxycholic Acid-d4 (CDCA-d4) is thedeuterium labeled Chenodeoxycholic Acid.Chenodeoxycholic Acid is a hydrophobic primarybile acid that activates nuclear receptors (FXR)involved in cholesterol metabolism.Purity: 9

14、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 50 mg HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d5.html Chenodeoxycholic HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d5.html HYPERLINK https:/www.MedChemE/chenodeoxy

15、cholic-acid-d5.html acid-d5 HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d5.html HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d9.html Chenodeoxycholic HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d9.html HYPERLINK https:/www.MedChemE/chenodeoxycholic-acid-d9.html Acid-d9(CDCA-d5

16、) Cat. No.: HY-76847S3 (CDCA-d9) Cat. No.: HY-76847S1Chenodeoxycholic acid-d5 (CDCA-d5) is thedeuterium labeled Chenodeoxycholic Acid.Chenodeoxycholic Acid is a hydrophobic primarybile acid that activates nuclear receptors (FXR)involved in cholesterol metabolism.Chenodeoxycholic Acid-d9 (CDCA-d9) is

17、 thedeuterium labeled Chenodeoxycholic Acid.Chenodeoxycholic Acid is a hydrophobic primarybile acid that activates nuclear receptors (FXR)involved in cholesterol metabolism.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

18、 mg HYPERLINK https:/www.MedChemE/Cilofexor.html Cilofexor HYPERLINK https:/www.MedChemE/Cilofexor.html HYPERLINK https:/www.MedChemE/dy268.html DY268(GS-9674) Cat. No.: HY-109083Cat. No.: HY-110267Cilofexor (GS-9674) is a potent, selective andorally active nonsteroidal FXR agonist with anEC of 43 n

19、M. Cilofexor has anti-inflammatory50and antifibrotic effects. Cilofexor has thepotential for primary sclerosing cholangitis (PSC)and nonalcoholic steatohepatitis (NASH) research.DY268 is a farnesoid X receptor (FXR) antagonist(IC =7.5 nM in a time-resolved FRET assay). It50inhibits FXR transactivati

20、on in a cell-based assaywith an IC50 value of 468 nM.Purity: 99.82%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Fexaramine.h

21、tml FexaramineCat. No.: HY-10912 HYPERLINK https:/www.MedChemE/Forskolin.html Forskolin(Coleonol; Colforsin) Cat. No.: HY-15371Fexaramine is a potent and selective FXR agonistwith an EC of 25 nM. Fexaramine has no50activity against hRXR, hPPAR, mPXR, hPXR,hLXR, hTR, hRAR, mCAR, mERR, and hVDRrecepto

22、rs.Forskolin (Coleonol) is a potent adenylate cyclaseactivator with an IC50 of 41 nM and an EC50 of0.5 M for type I adenylyl cyclase. Forskolin isalso an inducer of intracellular cAMPformation.Purity: 99.29%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 99.82%Clinical Da

23、ta: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-1.html FXR/TGR5 HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-1.html HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-1.html agonist HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-

24、1.html HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-1.html 1 HYPERLINK https:/www.MedChemE/fxr-tgr5-agonist-1.html HYPERLINK https:/www.MedChemE/Gly-_beta_-MCA.html Gly-MCACat. No.: HY-142159 Cat. No.: HY-114392FXR/TGR5 agonist 1 has agonist action on FXR andTGR5, and can be used for the treatment

25、 of fattyliver disease.Gly-MCA, a bile acid, is a potent, sable,intestine-selective and oral bioactive farnesoid Xreceptor (FXR) inhibitor that may be a candidatefor the treatment of metabolic disorders.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.11%Clinical Data: No

26、Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid.html Glyco-Obeticholic HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid.html HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid.html acid HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid.

27、html HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid-d5.html Glyco-obeticholic HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid-d5.html HYPERLINK https:/www.MedChemE/glyco-obeticholic-acid-d5.html acid-d5Cat. No.: HY-135400 Cat. No.: HY-135400SGlyco-obeticholic acid is an active metabolite

28、ofObeticholic acid. Obeticholic acid is a farnesoidX receptor (FXR) agonist.Glyco-obeticholic acid-d5 is the deuterium labeledGlyco-Obeticholic acid. Glyco-obeticholic acid isan active metabolite of Obeticholic acid.Obeticholic acid is a farnesoid X receptor (FXR)agonist.Purity: 98.0%Clinical Data:

29、No Development ReportedSize: 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/guggulsterone.html Guggulsterone HYPERLINK https:/www.MedChemE/guggulsterone.html HYPERLINK https:/www.MedChemE/GW-4064.html GW HYPERLINK https:/www.MedChemE/GW-4064.html

30、HYPERLINK https:/www.MedChemE/GW-4064.html 4064(Z/E-Guggulsterone) Cat. No.: HY-107738Cat. No.: HY-50108Guggulsterone is a plant sterol derived from thegum resin of the tree Commiphora wightii.GW 4064 is a potent FXR agonist with an EC of5065 nM.Purity: 99.83%Clinical Data: No Development ReportedSi

31、ze: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/INT-767.html INT-767 HYPERLINK https:/www.MedChemE/INT-767.html HYPERLINK https:/www.MedChemE/LY2562175.html LY2562175Cat.

32、No.: HY-12434 Cat. No.: HY-103704INT-767 is a dual farnesoid X receptor (FXR)/TGR5agonist with mean EC s of 30 and 630 nM,50respectively.LY2562175 is a potent and selective FXR agonist,with an EC of 193 nM.50Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurit

33、y: 99.26%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/ndb.html NDBCat. No.: HY-138937 HYPERLINK https:/www.MedChemE/nidufexor.html Nidufexor(LMB763) Cat. No.: HY-109096NDB is a selective human FXR (hFXR)antagonist that is effe

34、ctive in modulatingtranscription of FXR downstream genes. NDB can beused in anti-diabetes research.Nidufexor (LMB763) is an orally-available farnesoidX receptor (FXR) agonist for the research ofnonalcoholic steatohepatitis (NASH).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurit

35、y: 98.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nr1h4-activator-1.html NR1H4 HYPERLINK https:/www.MedChemE/nr1h4-activator-1.html HYPERLINK https:/www.MedChemE/nr1h4-activator-1.html activator HYPERLINK https:/www.MedChemE/nr1

36、h4-activator-1.html HYPERLINK https:/www.MedChemE/nr1h4-activator-1.html 1Cat. No.: HY-125996 HYPERLINK https:/www.MedChemE/INT-747.html Obeticholic HYPERLINK https:/www.MedChemE/INT-747.html HYPERLINK https:/www.MedChemE/INT-747.html acid(INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid) Cat. No.: HY

37、-12222NR1H4 activator 1 is a potent and selectiveFamesoid X Receptor (FXR) agonist, extractedfrom patent WO2018152171A1, example 4. NR1H4activator 1 shows strong FXR agonistic potencywith a EC value of 1 nM in a Human FXR (NR1H4)50Assay.Obeticholic acid (INT-747) is a potent, selectiveand orally act

38、ive FXR agonist with an EC of5099 nM. Obeticholic acid has anticholeretic andanti-inflammation effect. Obeticholic acid alsoinduces autophagy.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPE

39、RLINK https:/www.MedChemE/obeticholic-acid-d4.html Obeticholic HYPERLINK https:/www.MedChemE/obeticholic-acid-d4.html HYPERLINK https:/www.MedChemE/obeticholic-acid-d4.html Acid-d4Cat. No.: HY-12222S1 HYPERLINK https:/www.MedChemE/obeticholic-acid-d5.html Obeticholic HYPERLINK https:/www.MedChemE/ob

40、eticholic-acid-d5.html HYPERLINK https:/www.MedChemE/obeticholic-acid-d5.html acid-d5(INT-747-d5; 6-ECDCA-d5; 6-Ethylchenodeoxycholic acid-d5) Cat. No.: HY-12222SObeticholic Acid-d4 is the deuterium labeledObeticholic acid. Obeticholic acid (INT-747) is apotent, selective and orally active FXR agoni

41、stwith an EC of 99 nM. Obeticholic acid has50anticholeretic and anti-inflammation effect.Obeticholic acid also induces autophagy.Obeticholic acid-d5 (INT-747-d5) is the deuteriumlabeled Obeticholic acid. Obeticholic acid(INT-747) is a potent, selective and orally activeFXR agonist with an EC of 99 n

42、M. Obeticholic50acid has anticholeretic and anti-inflammationeffect. Obeticholic acid also induces autophagy.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg HYPERLINK https:/www.MedChemE/PX20606_trans_racemate.html

43、PX20606 HYPERLINK https:/www.MedChemE/PX20606_trans_racemate.html HYPERLINK https:/www.MedChemE/PX20606_trans_racemate.html trans HYPERLINK https:/www.MedChemE/PX20606_trans_racemate.html HYPERLINK https:/www.MedChemE/PX20606_trans_racemate.html racemate HYPERLINK https:/www.MedChemE/PX20606_trans_r

44、acemate.html HYPERLINK https:/www.MedChemE/Sevelamer.html Sevelamer(PX-102 trans racemate) Cat. No.: HY-100443ACat. No.: HY-13995PX20606 trans racemate (PX-102 trans racemate) isa FXR agonist with EC s of 32 and 34 nM for50FXR in FRET and M1H assay, respectively.Sevelamer is a phosphate binding drug

45、 used totreat hyperphosphatemia in patients with chronickidney disease; consists of polyallylamine that iscrosslinked with epichlorohydrin.Purity: 99.01%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 2 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/

46、Sevelamer-hydrochloride.html Sevelamer HYPERLINK https:/www.MedChemE/Sevelamer-hydrochloride.html HYPERLINK https:/www.MedChemE/Sevelamer-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Sevelamer-hydrochloride.html HYPERLINK https:/www.MedChemE/sevelamer-d5-n-hydrochloride.html Sevela

47、mer-(d5)n HYPERLINK https:/www.MedChemE/sevelamer-d5-n-hydrochloride.html HYPERLINK https:/www.MedChemE/sevelamer-d5-n-hydrochloride.html hydrochlorideCat. No.: HY-13995A Cat. No.: HY-13995ASSevelamer hydrochloride is a phosphate bindingdrug used to treat hyperphosphatemia in patientswith chronic ki

48、dney disease; consists ofpolyallylamine that is crosslinked withepichlorohydrin.Sevelamer-(d5)n hydrochloride is the deuteriumlabeled Sevelamer hydrochloride. Sevelamerhydrochloride is a phosphate binding drug used totreat hyperphosphatemia in patients with chronickidney disease; consists of polyall

49、ylamine that iscrosslinked with epichlorohydrin.Purity: 98.0%Clinical Data: LaunchedSize: 100 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/T0901317.html T0901317 HYPERLINK https:/ww

50、w.MedChemE/T0901317.html HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid.html Tauro-Obeticholic HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid.html HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid.html acidCat. No.: HY-10626 Cat. No.: HY-135399T0901317 is an orally active and highly s

51、electiveLXR agonist with an EC of 20 nM for LXR.50T0901317 activates FXR with an EC of 5 M.50T0901317 is ROR and ROR dual inverse agonistwith K values of 132 nM and 51 nM, respectively.iTauro-Obeticholic acid is an active metabolite ofObeticholic acid. Obeticholic acid is an orallybioavailable farne

52、soid-X receptor (FXR) agonist.Purity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid-d5-sodium.html Tauro-Obeticholic HYPERLINK https:/www.MedChemE/ta

53、uro-obeticholic-acid-d5-sodium.html HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid-d5-sodium.html acid-d5 HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid-d5-sodium.html HYPERLINK https:/www.MedChemE/tauro-obeticholic-acid-d5-sodium.html sodiumCat. No.: HY-135399S HYPERLINK https:/www.MedC

54、hemE/tauro-muricholic-acid-sodium.html Tauro-muricholic HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-sodium.html HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-sodium.html acid HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-sodium.html HYPERLINK https:/www.MedChemE/tauro-muricholic-

55、acid-sodium.html sodium(T-MCA sodium) Cat. No.: HY-135103Tauro 6-Ethlchenodeoxycholic Acid-d5 (sodium salt)is deuterium labeled Tauro-Obeticholic acid.Tauro-Obeticholic acid is an active metabolite ofObeticholic acid. Obeticholic acid is an orallybioavailable farnesoid-X receptor (FXR) agonist.Tauro

56、-muricholic Acid sodium (T-MCA sodium), aendogenous metabolite, is a competitive andreversible farnesoid X receptor (FXR) antagonist,with an IC of 40 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 95.0%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/ww

57、w.MedChemE/tauro-muricholic-acid-d4-sodium.html Tauro-muricholic HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-d4-sodium.html HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-d4-sodium.html acid-d4 HYPERLINK https:/www.MedChemE/tauro-muricholic-acid-d4-sodium.html HYPERLINK https:/www.MedCh

58、emE/tauro-muricholic-acid-d4-sodium.html sodiumCat. No.: HY-135103S HYPERLINK https:/www.MedChemE/Tropifexor.html Tropifexor(LJN452) Cat. No.: HY-107418Tauro-muricholic acid-d4 sodium is the deuteriumlabeled Tauro-muricholic acid sodium.Tauro-muricholic Acid sodium (T-MCA sodium), aendogenous metabo

59、lite, is a competitive andreversible farnesoid X receptor (FXR) antagonist,with an IC of 40 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgTropifexor (LJN452) is a highly potent agonist ofFXR with an EC of 0.2 nM.50Purity: 99.35%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg, 5 m

60、g, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/WAY-362450.html Turofexorate HYPERLINK https:/www.MedChemE/WAY-362450.html HYPERLINK https:/www.MedChemE/WAY-362450.html isopropyl HYPERLINK https:/www.MedChemE/WAY-362450.html HYPERLINK https:/www.MedChemE/Ursodiol.html Ursodeoxycholic H