PPAR-Agonists-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/PPAR.html PPARPeroxisome proliferator-activated receptorsPPARs (Peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes: PPAR, PPAR, and PPAR/. PPA

2、Rs play essential roles in the regulationof cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. AllPPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. Activation ofPP

3、AR- reduces triglyceride level and is involved in regulation of energy homeostasis. Activation of PPAR- enhances glucosemetabolism, whereas activation of PPAR-/ enhances fatty acids metabolism.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/PPAR.html PPAR HYPERLINK https:/www.MedChemE/Targets/P

4、PAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/PPAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/PPAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html Antagonists, HYPERLINK https:

5、/www.MedChemE/Targets/PPAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html Activators HYPERLINK https:/www.MedChemE/Targets/PPAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html & HYPERLINK https:/www.MedChemE/Targets/PPAR.html HYPERLINK https:/www.MedChemE/Targets/PPAR.html Modulators HYPE

6、RLINK https:/www.MedChemE/s-coriolic-acid.html (S)-Coriolic HYPERLINK https:/www.MedChemE/s-coriolic-acid.html HYPERLINK https:/www.MedChemE/s-coriolic-acid.html acid(13(S)-HODE) Cat. No.: HY-113884B HYPERLINK https:/www.MedChemE/10-nitrolinoleic-acid.html 10-Nitrolinoleic HYPERLINK https:/www.MedCh

7、emE/10-nitrolinoleic-acid.html HYPERLINK https:/www.MedChemE/10-nitrolinoleic-acid.html acidCat. No.: HY-113473(S)-Coriolic acid (13(S)-HODE), the product of15-lipoxygenase (15-LOX) metabolism of linoleicacid, functions as the endogenous ligand toactivate PPAR.10-Nitrolinoleic acid is a potent perox

8、isomeproliferator-activated receptor (PPAR)agonist. 10-Nitrolinoleic acid competes with3HRosiglitazone for binding to PPAR-, with anIC of 0.22 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.M

9、edChemE/11-cis-retinoic-acid-d5.html 11-cis-Retinoic HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html Acid-d5 HYPERLINK https:/www.MedChemE/11-cis-retinoic-acid-d5.html HYPERLINK https:/www.MedChemE/13-oxo-9e-11e-octadecadienoic-ac

10、id.html 13-Oxo-9E,11E-octadecadienoic HYPERLINK https:/www.MedChemE/13-oxo-9e-11e-octadecadienoic-acid.html HYPERLINK https:/www.MedChemE/13-oxo-9e-11e-octadecadienoic-acid.html acidCat. No.: HY-14649S2 Cat. No.: HY-N509711-cis-Retinoic Acid-d5 is the deuterium labeledRetinoic acid. Retinoic acid is

11、 a metabolite ofvitamin A that plays important roles in cellgrowth, differentiation, and organogenesis.13-Oxo-9E,11E-octadecadienoic acid, an isomer of9-oxo-ODA, is a potent PPAR activator derivedfrom tomato juice. 13-Oxo-9E,11E-octadecadienoicacid decreases plasma and hepatic triglyceride inobese d

12、iabetic mice.Purity: 98%Clinical Data: No Development ReportedSize: 500 g, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/15-Deoxy-12,14-prostaglandin.html 15-Deoxy-12,14-prostaglandin HYPERLINK https:/www.MedChemE/15-Deoxy-12,14-prostagla

13、ndin.html HYPERLINK https:/www.MedChemE/15-Deoxy-12,14-prostaglandin.html J2(15d-PGJ2; 15-Deoxy-12,14-PGJ2) Cat. No.: HY-108568 HYPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d4.html 15-Deoxy-12,14-prostaglandin HYPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d4.html HYP

14、ERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d4.html J2-d4(15d-PGJ2-d4; 15-Deoxy-12,14-PGJ2-d4) Cat. No.: HY-108568S15-Deoxy-12,14-prostaglandin J2 (15d-PGJ2) is acyclopentenone prostaglandin and a metabolite ofPGD2. 15-Deoxy-12,14-prostaglandin J2 is aselective PPAR (EC of 2 M) and a

15、covalent50PPAR agonist.15-Deoxy-12,14-prostaglandin J2-d4 (15d-PGJ2-d4)is the deuterium labeled15-Deoxy-12,14-prostaglandin J2.15-Deoxy-12,14-prostaglandin J2 (15d-PGJ2) is acyclopentenone prostaglandin and a metabolite ofPGD2.Purity: 96.0%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%C

16、linical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d9.html 15-Deoxy-12,14-Prostaglandin HYPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d9.html HYPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d9.html J2-d9 H

17、YPERLINK https:/www.MedChemE/15-deoxy-12-14-prostaglandin-j2-d9.html HYPERLINK https:/www.MedChemE/4-O-Methyl_honokiol.html 4-O-Methyl HYPERLINK https:/www.MedChemE/4-O-Methyl_honokiol.html HYPERLINK https:/www.MedChemE/4-O-Methyl_honokiol.html honokiol(15d-PGJ2-d9; 15-Deoxy-12,14-PGJ2-d9) Cat. No.:

18、 HY-108568S1Cat. No.: HY-U0045015-Deoxy-12,14-Prostaglandin J2-d9 (15d-PGJ2-d9)is the deuterium labeled15-Deoxy-12,14-prostaglandin J2.15-Deoxy-12,14-prostaglandin J2 (15d-PGJ2) is acyclopentenone prostaglandin and a metabolite ofPGD2.4-O-Methyl honokiol is a natural neolignanisolated from Magnolia

19、officinalis, acts as aPPAR agonist, and inhibtis NF-B activity, usedfor cancer and inflammation research.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/5-Aminosalicylic-acid.html 5-A

20、minosalicylic HYPERLINK https:/www.MedChemE/5-Aminosalicylic-acid.html HYPERLINK https:/www.MedChemE/5-Aminosalicylic-acid.html Acid HYPERLINK https:/www.MedChemE/5-Aminosalicylic-acid.html HYPERLINK https:/www.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html 5-Aminosalicylic HYPERLINK https:/ww

21、w.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html Acid-D3 HYPERLINK https:/www.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html hydrochloride H

22、YPERLINK https:/www.MedChemE/5-aminosalicylic-acid-d3-hydrochloride.html (Mesalamine-D3(Mesalamine; 5-ASA; Mesalazine) Cat. No.: HY-15027 hydrochloride; 5-ASA-D3 hydrochloride; ) Cat. No.: HY-15027S5-Aminosalicylic acid (Mesalamine) acts as aspecific PPAR agonist and also inhibitsp21-activated kinas

23、e 1 (PAK1) and NF-B.5-Aminosalicylic Acid-D3 (Mesalamine-D3)hydrochloride is the deuterium labeled5-Aminosalicylic Acid. 5-Aminosalicylic acid(Mesalamine) hydrochloride acts as a specificPPAR agonist and also inhibits p21-activatedkinase 1 (PAK1) and NF-B.Purity: 98.0%Clinical Data: LaunchedSize: 10

24、 mM 1 mL, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/Adelmidrol.html Adelmidrol HYPERLINK https:/www.MedChemE/Adelmidrol.html HYPERLINK https:/www.MedChemE/agrimol-b.html Agrim

25、ol HYPERLINK https:/www.MedChemE/agrimol-b.html HYPERLINK https:/www.MedChemE/agrimol-b.html BCat. No.: HY-B1026 Cat. No.: HY-N0704Adelmidrol exerts important anti-inflammatoryeffects that are partly dependent on PPAR.Adelmidrol reduces NF-B translocation, andCOX-2 expression.Agrimol B is a polyphen

26、ol derived fromAgrimonia pilosa Ledeb, suppresses adipogenesisvia inducing SIRT1 translocation and expression,and reducing PPAR expression.Purity: 98.0%Clinical Data: Phase 3Size: 10 mM 1 mL, 100 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/al

27、eglitazar.html Aleglitazar(R1439; RO0728804) Cat. No.: HY-14728 HYPERLINK https:/www.MedChemE/alpinetin.html AlpinetinCat. No.: HY-N0625AAleglitazar (R1439) is a potent dual PPAR/agonist, with IC s of 38 nM and 19 nM for human50PPARa and PPAR, respectively. Aleglitazar can beused for the research of

28、 type II diabetes.Alpinetin is a flavonoid isolated from Alpiniakatsumadai Hayata, activates activates PPAR-,with potent anti-inflammatory activity.Purity: 99.30%Clinical Data: Phase 3Size: 5 mgPurity: 99.89%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 20 mg HYPERLINK https:/

29、www.MedChemE/am3102.html AM3102Cat. No.: HY-129683 HYPERLINK https:/www.MedChemE/amg131.html AMG131(INT131) Cat. No.: HY-117103AM3102 is an oleoylethanolamide (OEA) analog.AM3102 is an endogenous high-affinity PPAR-alphaagonist. AM3102 resists enzymatic hydrolysis,activates PPAR-alpha with high pote

30、ncy in vitro,and persistently reduces feeding when administeredin vivo either parenterally or orally.AMG131 (INT131), a potent and highly selectivePPAR partial agonist, binds to PPAR anddisplaces Rosiglitazone with a K of 10 nM.iAMG131 can be used for research of type-2 diabetesmellitus (T2DM).Purit

31、y: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.13%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/angeloylgomisin-h.html Angeloylgomisin HYPERLINK https:/www.MedChemE/angeloylgomisin-h.html HYPERLINK https:/www.MedCh

32、emE/angeloylgomisin-h.html H HYPERLINK https:/www.MedChemE/angeloylgomisin-h.html HYPERLINK https:/www.MedChemE/ankaflavin.html AnkaflavinCat. No.: HY-N2209 Cat. No.: HY-N6642Angeloylgomisin H, as a major lignin extract ofSchisandra rubriflora, has the potential to improveinsulin-stimulated glucose

33、uptake by activatingPPAR-.Ankaflavin, isolated from Monascus-Fermented redrice, is a PPAR agonist with anti-inlfammatoryactivity. Ankaflavin exhibits selective cytotoxiceffect and induces cell death on cancer cells.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 95.0%Clinic

34、al Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/MBX_102.html Arhalofenate HYPERLINK https:/www.MedChemE/MBX_102.html HYPERLINK https:/www.MedChemE/Astaxanthin.html Astaxanthin(MBX 102; JNJ 39659100) Cat. No.: HY-14831Cat. No.: HY-B2163Arhalofenate (M

35、BX 102) is a selective partialagonist of peroxisome proliferator-activatedreceptor (PPAR)-, used for the treatment of type2 diabetes.Astaxanthin, a red dietary carotenoid isolatedfrom Haematococcus pluvialis, is a modulator ofPPAR and a potent antioxidant withantiproliferative, neuroprotective andan

36、ti-inflammatory activity.Purity: 98%Clinical Data: Phase 3Size: 1 mg, 5 mgPurity: 98.0%Clinical Data: LaunchedSize: 5 mg, 10 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/atra-biotin.html ATRA-biotin(Biotin-ATRA-conjugate) Cat. No.: HY-141793 HYPERLINK https:/www.MedChemE/AVE-8134.html AVE-8134Cat.

37、 No.: HY-U00014ATRA-biotin (Biotin-ATRA-conjugate) is abiotin-conjugated ATRA. ATRA-biotin can be used totrack ATRA in cells or a given tissue.AVE-8134 is a potent PPAR agonist, with EC50values of 100 and 3000 nM for human and rodentPPAR receptor, respectively.Purity: 98%Clinical Data: No Developmen

38、t ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/azd-9574.html AZD-9574Cat. No.: HY-145804 HYPERLINK https:/www.MedChemE/balaglitazone.html Balaglitazone(DRF 2593; NN 2344) Cat. No.: HY-16086AZD9574 is a potent, blood-brain bar

39、rier(BBB) penetrant and PARP1 selectiveinhibitor. AZD9574 can be used for primary andsecondary brain malignancies research.Balaglitazone is a selective partial PPARagonist with an EC of 1.351 M for human50PPAR.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPu

40、rity: 99.97%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Bezafibrate.html Bezafibrate(BM15075) Cat. No.: HY-B0637 HYPERLINK https:/www.MedChemE/bezafibrate-d4.html Bezafibrate-d4(BM15075-d4) Cat. No.: HY-B0637S1Bezafibrate is an agonist of PPAR, wi

41、th EC s50of 50 M, 60 M, 20 M for human PPAR, PPARand PPAR, and 90 M, 55 M, 110 M for murinePPAR, PPAR and PPAR, respectively;Bezafibrate is used as an hypolipidemic agent.Bezafibrate-d4 is deuterium labeled Bezafibrate.Bezafibrate is an agonist of PPAR, with EC50s of50 M, 60 M, 20 M for human PPAR,

42、PPAR andPPAR, and 90 M, 55 M, 110 M for murine PPAR,PPAR and PPAR, respectively; Bezafibrate is usedas an hypolipidemic agent.Purity: 99.43%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bezafibrate-d6.ht

43、ml Bezafibrate-d6 HYPERLINK https:/www.MedChemE/bezafibrate-d6.html HYPERLINK https:/www.MedChemE/bilobetin.html BilobetinCat. No.: HY-B0637S Cat. No.: HY-N2118Bezafibrate-d6 is the deuterium labeledBezafibrate.Bilobetin, an active component of Ginkgo biloba, canreduce blood lipids and improve the e

44、ffects ofinsulin.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.30%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/BMS-687453.html BMS-687453 HYPERLINK https:/www.MedChemE/BMS-687453.html HYPERLINK https:/www.MedChemE/bocidelp

45、ar.html BocidelparCat. No.: HY-10678 Cat. No.: HY-134377BMS-687453 is a potent and selective PPARagonist, with an EC50 and IC50 of 10 nM and 260nM for human PPAR and 4100 nM and 15000 nMfor PPAR in PPAR-GAL4 transactivation assays.Bocidelpar is a modulator of peroxisomeproliferator-activated recepto

46、r delta (PPAR-).Bocidelpar improves mitochondrial biogenesis andfunction in Duchenne Muscular Dystrophy (DMD)muscle cells (extracted from patentWO2017062468A1, compound 2b).Purity: 98.58%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data

47、: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/caulophyllogenin.html CaulophyllogeninCat. No.: HY-N7687 HYPERLINK https:/www.MedChemE/CDDO-Im.html CDDO-Im(RTA-403; TP-235; CDDO-Imidazolide) Cat. No.: HY-15725Caulophyl

48、logenin is a triterpene saponin extractedfrom M. polimorpha. Caulophyllogenin is apartial PPAR agonist, with anEC of12.6M. Caulophyllogenin can be used50for the research of type-2 diabetes, obesity,metabolic syndrome and inflammation.CDDO-Im (RTA-403) is an activator of Nrf2 andPPAR, with Ks of 232

49、and 344 nM for PPAR andiPPAR.Purity: 98%Clinical Data: No Development ReportedSize: 1 mgPurity: 98.19%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cefminox-sodium.html Cefminox HYPERLINK https:/www.MedChemE/cefminox-sodium.html HYPERLINK https:/ww

50、w.MedChemE/cefminox-sodium.html sodium(MT-141) Cat. No.: HY-128932 HYPERLINK https:/www.MedChemE/Chiglitazar.html Chiglitazar(Carfloglitazar) Cat. No.: HY-106266Cefminox sodium (MT-141) is a semisyntheticcephamycin, which exhibits a broad spectrum ofantibacterial activity.Chiglitazar (Carfloglitazar

51、) is a PPAR/ dualagonist, with EC s of 1.2, 0.08, 1.7 M for50PPAR, PPAR and PPAR, respectively.Purity: 99.83%Clinical Data: LaunchedSize: 25 mgPurity: 98%Clinical Data: Phase 3Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Choline-Fenofibrate.html Choline HYPERLINK https:/www.

52、MedChemE/Choline-Fenofibrate.html HYPERLINK https:/www.MedChemE/Choline-Fenofibrate.html Fenofibrate(ABT-335) Cat. No.: HY-14739 HYPERLINK https:/www.MedChemE/ciglitazone.html Ciglitazone(ADD-3878; U-63287) Cat. No.: HY-W011220Choline Fenofibrate (ABT-335), a choline salt ofFenofibric acid (HY-B0760

53、), releases freeFenofibric acid in the gastrointestinal tract.Fenofibric acid is a PPAR activator withantihyperlipidemic effect.Ciglitazone is a potent and selective PPARagonist (EC =3 M). Ciglitazone inhibits50proliferation and differentiation of th17 cells.Ciglitazone is a hypoglycemic agent orall

54、y activein the obese-hyperglycemic animal models.Purity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg HYPERLINK https:/www.MedChemE/cinnamyl-alcohol.html Cinnamyl HYPERLINK https:/www.MedChemE/cinnamyl-alcohol.html HYPERLINK

55、https:/www.MedChemE/cinnamyl-alcohol.html Alcohol HYPERLINK https:/www.MedChemE/cinnamyl-alcohol.html HYPERLINK https:/www.MedChemE/Ciprofibrate.html CiprofibrateCat. No.: HY-Y0078(Win35833) Cat. No.: HY-B0664Cinnamyl Alcohol is an active component fromchestnut flower, inhibits increased PPARexpress

56、ion, with anti-obesity activity.Ciprofibrate (Win35833) is a potent peroxisomeproliferator and increases the phosphorylationlevel of the PPARalpha. Ciprofibrate acts as anorally active hypolipidaemic agent and can be usedfor the research of primary hyperlipidaemias.Purity: 99.34%Clinical Data: No De

57、velopment ReportedSize: 5 mgPurity: 99.79%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 500 mg HYPERLINK https:/www.MedChemE/Ciprofibrate-D6.html Ciprofibrate HYPERLINK https:/www.MedChemE/Ciprofibrate-D6.html HYPERLINK https:/www.MedChemE/Ciprofibrate-D6.html D6 HYPERLINK https:/www.MedChemE/Cip

58、rofibrate-D6.html HYPERLINK https:/www.MedChemE/ciprofibrate-impurity-a.html Ciprofibrate HYPERLINK https:/www.MedChemE/ciprofibrate-impurity-a.html HYPERLINK https:/www.MedChemE/ciprofibrate-impurity-a.html impurity HYPERLINK https:/www.MedChemE/ciprofibrate-impurity-a.html HYPERLINK https:/www.Med

59、ChemE/ciprofibrate-impurity-a.html ACat. No.: HY-B0664S Cat. No.: HY-133777Ciprofibrate D6 is deuterium labeled Ciprofibrate.Ciprofibrate (Win35833) is a potent peroxisomeproliferator, increases the phosphorylation levelof the PPARalpha.Ciprofibrate impurity A is an impurity ofCiprofibrate. Ciprofib

60、rate (Win35833) is a potentperoxisome proliferator, increases thephosphorylation level of the PPARalpha.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/2-4-ethenylphenoxy-2-