AMPK-Activators-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/AMPK.html AMPKAMP-activated protein kinaseAMPK (AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. It consists of three proteins(subunits) that together make a functional enzyme. The net effect of AMPK activation is sti

2、mulation of hepatic fatty acid oxidationandketogenesis, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis andlipogenesis, stimulation of skeletal muscle fatty acid oxidation and muscle glucose uptake by pancreatic beta-cells. AMPK acts as

3、 ametabolic master switch regulating several intracellular systems including the cellular uptake of glucose, the -oxidation of fattyacids and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/AMPK.html AMPK HYPERLINK https:/www.MedC

4、hemE/Targets/AMPK.html HYPERLINK https:/www.MedChemE/Targets/AMPK.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/AMPK.html HYPERLINK https:/www.MedChemE/Targets/AMPK.html & HYPERLINK https:/www.MedChemE/Targets/AMPK.html HYPERLINK https:/www.MedChemE/Targets/AMPK.html Activators HYPERLINK htt

5、ps:/www.MedChemE/10z-hymenialdisine.html 10Z-Hymenialdisine(Z)-Hymenialdisine; Hymenialdisine) Cat. No.: HY-N6794 HYPERLINK https:/www.MedChemE/3-alpha-hydroxymogrol.html 3-HydroxymogrolCat. No.: HY-N691310Z-Hymenialdisine (Z)-Hymenialdisine) is anatural bioactive pyrrole alkaloid.10Z-Hymenialdisine

6、 is a pan kinase inhibitor, andhas anticancer activities.3-Hydroxymogrol is a triterpenoid isolated fromSiraitia grosvenorii Swingle, acts as a potentAMPK activator, and enhances AMPKphosphorylation.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.47%Clinical Data: No Deve

7、lopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/7-Methoxyisoflavone.html 7-Methoxyisoflavone HYPERLINK https:/www.MedChemE/7-Methoxyisoflavone.html HYPERLINK https:/www.MedChemE/A-769662.html A-769662Cat. No.: HY-N6631 Cat. No.: HY-506627-Methoxyisoflavone is an isoflavone derivativea

8、nd also an activator of adenosinemonophosphate-activated protein kinase (AMPK).A-769662 is a potent, reversible AMPK activatorwith EC of 0.8 M.50Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mgPurity: 98.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

9、mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AICAR.html AICAR(Acadesine; AICA Riboside) Cat. No.: HY-13417 HYPERLINK https:/www.MedChemE/AICAR-phosphate.html AICAR HYPERLINK https:/www.MedChemE/AICAR-phosphate.html HYPERLINK https:/www.MedChemE/AICAR-phosphate.html phosphate(Acadesine phosphate;

10、AICA Riboside phosphate) Cat. No.: HY-13417AAICAR (Acadesine) is an adenosine analog and aAMPK activator. AICAR regulates the glucose andlipid metabolism, and inhibits proinflammatorycytokines and iNOS production. AICAR is also anautophagy, YAP and mitophagy inhibitor.AICAR phosphate (Acadesine phos

11、phate) is anadenosine analog and a AMPK activator. AICARphosphate regulates the glucose and lipidmetabolism, and inhibits proinflammatory cytokinesand iNOS production. AICAR phosphate is also anautophagy, YAP and mitophagy inhibitor.Purity: 99.92%Clinical Data: Phase 3Size: 50 mg, 100 mg, 200 mg, 50

12、0 mgPurity: 99.49%Clinical Data: Phase 3Size: 10 mM 1 mL, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/amarogentin.html Amarogentin HYPERLINK https:/www.MedChemE/amarogentin.html HYPERLINK https:/www.MedChemE/2-Benzofurancarboxamide,_N-1-_4-pyridinylmethyl_-4-piperidinyl-5-1-4-_triflu

13、oromethyl_phenyl-4-piperidinyloxy-.html AMPK HYPERLINK https:/www.MedChemE/2-Benzofurancarboxamide,_N-1-_4-pyridinylmethyl_-4-piperidinyl-5-1-4-_trifluoromethyl_phenyl-4-piperidinyloxy-.html HYPERLINK https:/www.MedChemE/2-Benzofurancarboxamide,_N-1-_4-pyridinylmethyl_-4-piperidinyl-5-1-4-_trifluoro

14、methyl_phenyl-4-piperidinyloxy-.html activator HYPERLINK https:/www.MedChemE/2-Benzofurancarboxamide,_N-1-_4-pyridinylmethyl_-4-piperidinyl-5-1-4-_trifluoromethyl_phenyl-4-piperidinyloxy-.html HYPERLINK https:/www.MedChemE/2-Benzofurancarboxamide,_N-1-_4-pyridinylmethyl_-4-piperidinyl-5-1-4-_trifluo

15、romethyl_phenyl-4-piperidinyloxy-.html 1Cat. No.: HY-N2447 Cat. No.: HY-U00292Amarogentin is a secoiridoid glycoside that ismainly extracted from Swertia and Gentianaroots. Amarogentin exhibits many biologicaleffects, including anti-oxidative, anti-tumour,and anti-diabetic activities.AMPK activator

16、1 is an AMPK activator extractedfrom patent WO2013116491A1, compound No.1-75, hasan EC of 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/buformin-hydrochloride.html Buformin HYPERLINK https:/www.MedChemE/buformin-hydrochloride.html HYPERLINK https:/www.MedChe

17、mE/buformin-hydrochloride.html hydrochloride(1-Butylbiguanide hydrochloride) Cat. No.: HY-B2099A HYPERLINK https:/www.MedChemE/buformin-d9-hydrochloride.html Buformin-d9 HYPERLINK https:/www.MedChemE/buformin-d9-hydrochloride.html HYPERLINK https:/www.MedChemE/buformin-d9-hydrochloride.html hydrochl

18、oride(1-Butylbiguanide-d9 hydrochloride) Cat. No.: HY-B2099SBuformin hydrochloride (1-Butylbiguanidehydrochloride), a potent AMPK activator, acts asan orally active biguanide antidiabetic agent.Buformin hydrochloride decreases hepaticgluconeogenesis and lowers blood glucoseproduction in vivo.Buformi

19、n-d9 (1-Butylbiguanide-d9) hydrochloride isthe deuterium labeled Buformin. Buformin(1-Butylbiguanide), a potent AMPK activator, actsas an orally active biguanide antidiabetic agent.Buformin decreases hepatic gluconeogenesis andlowers blood glucose production in vivo.Purity: 98.62%Clinical Data: No D

20、evelopment ReportedSize: 250 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Chitosan_oligosaccharide_COS.html Chitosan HYPERLINK https:/www.MedChemE/Chitosan_oligosaccharide_COS.html HYPERLINK https:/www.MedChemE/Chitosan_oligosaccharide_COS

21、.html oligosaccharide HYPERLINK https:/www.MedChemE/Chitosan_oligosaccharide_COS.html HYPERLINK https:/www.MedChemE/cimiracemoside-c.html Cimiracemoside HYPERLINK https:/www.MedChemE/cimiracemoside-c.html HYPERLINK https:/www.MedChemE/cimiracemoside-c.html C(COS) Cat. No.: HY-112108 (Cimicifugoside

22、M) Cat. No.: HY-N6971Chitosan oligosaccharide (COS) is an oligomer of-(14)-linked D-glucosamine. Chitosanoligosaccharide (COS) activates AMPK andinhibits inflammatory signaling pathways includingNF-B and MAPK pathways.Cimiracemoside C is an active component ofCimicifuga racemosa, activates AMPK, has

23、the potential activity against diabetes.Purity: 91.0%Clinical Data: No Development ReportedSize: 10 mg(10 mg mL in Water), 500 mg, 1 g, 5 gPurity: 99.55%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/coh-sr4.html COH-SR4 HYPERLINK https:/www.MedChemE/coh-sr4.ht

24、ml HYPERLINK https:/www.MedChemE/d942.html D942Cat. No.: HY-124822 Cat. No.: HY-131958COH-SR4 is an AMPK activator. COH-SR4 showspotent anti-proliferative activities againstleukemia, melanoma, breast and lung cancers.COH-SR4 inhibits adipocyte differentiation viaAMPK activation.D942 is a cell penetr

25、ant AMPK activator andpartially inhibits the mitochondrial complex I. Inmultiple myeloma cells, D942 inhibits cell growth.Purity: 99.73%Clinical Data: No Development ReportedSize: 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www

26、.MedChemE/Danthron.html Danthron(Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone) Cat. No.: HY-B0923 HYPERLINK https:/www.MedChemE/danthron-d6.html Danthron-d6(Dantron-d6; Chrysazin-d6; 1,8-Dihydroxyanthraquinone-d6) Cat. No.: HY-B0923SDanthron is a natural product extracted from thetraditional Chine

27、se medicine rhubarb. Danthronfunctions in regulating glucose and lipidmetabolism by activating AMPK.Danthron-d6 (Dantron-d6) is the deuterium labeledDanthron. Danthron is a natural product extractedfrom the traditional Chinese medicine rhubarb.Danthron functions in regulating glucose and lipidmetabo

28、lism by activating AMPK.Purity: 98.70%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/demethyleneberberine.html DemethyleneberberineCat. No.: HY-N0592 HYPERLINK https:/www.MedChemE/dorsomorphin.html Dorso

29、morphin(Compound C; BML-275) Cat. No.: HY-13418ADemethyleneberberine is a naturalmitochondria-targeted antioxidant.Demethyleneberberine alleviates mice colitis andinhibits the inflammatory responses by inhibitingNF-B pathway and regulating the balance of Thcells.Dorsomorphin (Compound C) is a select

30、ive andATP-competitive AMPK inhibitor (K=109 nM inithe absence of AMP). Dorsomorphin (BML-275)selectively inhibits BMP type I receptors ALK2,ALK3, and ALK6. Dorsomorphin induces autophagy.Purity: 98.09%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.91%Clinical Data: No

31、 Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Dorsomorphin-dihydrochloride.html Dorsomorphin HYPERLINK https:/www.MedChemE/Dorsomorphin-dihydrochloride.html HYPERLINK https:/www.MedChemE/Dorsomorphin-dihydrochloride.html dihydrochloride(Compound C di

32、hydrochloride; BML-275 dihydrochloride) Cat. No.: HY-13418 HYPERLINK https:/www.MedChemE/Doxorubicin.html Doxorubicin(Hydroxydaunorubicin) Cat. No.: HY-15142ADorsomorphin dihydrochloride (BML-275dihydrochloride; Compound C dihydrochloride) is apotent, selective and ATP-competitive AMPKinhibitor, wit

33、h a K of 109 nM.iDoxorubicin (Hydroxydaunorubicin), a cytotoxicanthracycline antibiotic, is an anti-cancerchemotherapy agent. Doxorubicin inhibitstopoisomerase II with an IC of 2.67 M, thus50stopping DNA replication.Purity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 5

34、0 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/Doxorubicin-hydrochloride.html Doxorubicin HYPERLINK https:/www.MedChemE/Doxorubicin-hydrochloride.html HYPERLINK https:/www.MedChemE/Doxorubicin-hydrochloride.html hydrochloride HYPERLINK https:/www

35、.MedChemE/Doxorubicin-hydrochloride.html HYPERLINK https:/www.MedChemE/eb-3d.html EB-3D(Hydroxydaunorubicin hydrochloride) Cat. No.: HY-15142Cat. No.: HY-115463Doxorubicin (Hydroxydaunorubicin) hydrochloride, acytotoxic anthracycline antibiotic, is ananti-cancer chemotherapy agent. Doxorubicinhydroc

36、hloride is a potent human DNA topoisomeraseI and topoisomerase II inhibitor with IC s of500.8 M and 2.67 M, respectively.EB-3D is a potent and selective choline kinase (ChoK) inhibitor, with an IC of 1 M for50ChoK1. EB-3D exerts effects on ChoK expression,AMPK activation, apoptosis, endoplasmicretic

37、ulum stress and lipid metabolism.Purity: 99.47%Clinical Data: LaunchedSize: 10 mM 1 mL, 50 mg, 100 mg, 200 mg, 500 mg, 1 gPurity: 98.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/etilefrine.html Etilefrine HYPERLINK https:/www.MedChemE/et

38、ilefrine.html HYPERLINK https:/www.MedChemE/euphorbiasteroid.html EuphorbiasteroidCat. No.: HY-A0144 Cat. No.: HY-N2032Etilefrine(3-2-(ethylamino)-1-hydroxyethylphenol) is an adrenergic agonist. Etilefrine also is an AMPKactivator. Etilefrine can be used for the researchof postural hypotension.Eupho

39、rbiasteroid is a tricyclic diperpene ofEuphorbia lathyris L., inhibits tyrosinase, andincreases the phosphorylation of AMPK, withanti-cancer, anti-virus, anti-obesity andmultidrug resistance-modulating effect.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.76%Clinical Data: No Developme

40、nt ReportedSize: 5 mg, 10 mg, 20 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/EX229.html EX229 HYPERLINK https:/www.MedChemE/EX229.html HYPERLINK https:/www.MedChemE/Flufenamic-acid.html Flufenamic HYPERLINK https:/www.MedChemE/Flufenamic-acid.html HYPER

41、LINK https:/www.MedChemE/Flufenamic-acid.html acidCat. No.: HY-112769 Cat. No.: HY-B1221EX229, a Benzimidazole derivative, is a potent andallosteric activator of AMP-activated proteinkinase (AMPK), with K s of 0.06 M, 0.06 Mdand 0.51 M for 111, 211 and 121 inbiolayer interferometry, respectively.Flu

42、fenamic acid is a non-steroidalanti-inflammatory agent, inhibits cyclooxygenase(COX), activates AMPK, and also modulates ionchannels, blocking chloride channels and L-typeCa2+ channels, modulating non-selective cationchannels (NSC), activatingPurity: 98.45%Clinical Data: No Development ReportedSize:

43、 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.85%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg HYPERLINK https:/www.MedChemE/flufenamic-acid-d4.html Flufenamic HYPERLINK https:/www.MedChemE/flufenamic-acid-d4.html HYPERLINK https:/www.MedChemE/flufenamic-acid-d4.html acid-d4 HYPERLINK https:/ww

44、w.MedChemE/flufenamic-acid-d4.html HYPERLINK https:/www.MedChemE/galegine-hydrochloride.html Galegine HYPERLINK https:/www.MedChemE/galegine-hydrochloride.html HYPERLINK https:/www.MedChemE/galegine-hydrochloride.html hydrochlorideCat. No.: HY-B1221S Cat. No.: HY-N0930BFlufenamic acid-d4 is deuteriu

45、m labeled Flufenamicacid.Galegine hydrochloride, a guanidine derivative,contributes to weight loss in mice. Guanidinehydrochloride is the compound derived from G.officinalis, which gave rise to the biguanides,metformin and phenformin.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgP

46、urity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Ginkgolide-C.html Ginkgolide HYPERLINK https:/www.MedChemE/Ginkgolide-C.html HYPERLINK https:/www.MedChemE/Ginkgolide-C.html C(BN-52022; Ginkgolide-C) Cat. No.: HY-N0785 HYPERLINK https:/www.MedChemE/gomi

47、sin-j.html Gomisin HYPERLINK https:/www.MedChemE/gomisin-j.html HYPERLINK https:/www.MedChemE/gomisin-j.html JCat. No.: HY-N0385Ginkgolide C is a flavone isolated from Ginkgobiloba leaves, possessing multiple biologicalfunctions, such as decreasing platelet aggregationand ameliorating Alzheimer dise

48、ase.Gomisin J is a small molecular weight lignan foundin Schisandra chinensis and has been demonstrated tohave vasodilatory activity.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 99.67%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 m

49、g HYPERLINK https:/www.MedChemE/GSK-690693.html GSK-690693 HYPERLINK https:/www.MedChemE/GSK-690693.html HYPERLINK https:/www.MedChemE/gsk621.html GSK621Cat. No.: HY-10249 Cat. No.: HY-100548GSK-690693 is an ATP-competitive pan-Aktinhibitor with IC s of 2 nM, 13 nM, 9 nM for50Akt1, Akt2 and Akt3, re

50、spectively. GSK-690693is also an AMPK inhibitor, affects Unc-51-likeautophagy activating kinase 1 (ULK1) activity androbustly inhibits STING-dependent IRF3 activation.GSK621 is a specific AMPK activator, with IC50values of 13-30 M for AML cells. GSK621 inducesautophagy and apoptosis. GSK621 induces

51、eiF2phosphorylation-a hallmark of UPR activation.Purity: 98.40%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.82%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/hl271.html HL271 HYPERLINK https:/www.MedChemE/hl271.html

52、 HYPERLINK https:/www.MedChemE/HTH-01-015.html HTH-01-015(IM156 hydrochloride; HL156A hydrochloride) Cat. No.: HY-136093Cat. No.: HY-12334HL271 (IM156 hydrochloride; HL156A hydrochloride),a chemical derivative of Metformin (HY-B0627), isa potent AMPK activator that increases AMPKphosphorylation. HL2

53、71 attenuates aging-associatedcognitive impairment in animal model.HTH-01-015 is a selective NUAK1/ARK5 inhibitor(IC is 100 nM). HTH-01-015 inhibits NUAK1 with50100-fold higher potency than NUAK2 (IC50 of10 M).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.18%Clinical Da

54、ta: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/im156.html IM156(HL156A; HL271 acetate) Cat. No.: HY-136093A HYPERLINK https:/www.MedChemE/iqz23.html IQZ23Cat. No.: HY-133556IM156 (HL156A; HL271 acetate), a chemicalderivative of Met

55、formin (HY-B0627), is a potentand orally active AMPK activator that increasesAMPK phosphorylation. IM156 attenuatesaging-associated cognitive impairment in animalmodel.IQZ23 inhibits adipocyte differentiation viaAMPK pathway activation. IQZ23 exerts a highefficacy in decreasing the triglyceride leve

56、l(EC =0.033 M) in 3T3-L1 adipocytes. IQZ23 could50be used for the research of obesity and relatedmetabolic disorders.Purity: 99.80%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/kahweol

57、.html Kahweol HYPERLINK https:/www.MedChemE/kahweol.html HYPERLINK https:/www.MedChemE/karanjin.html KaranjinCat. No.: HY-N6258 Cat. No.: HY-N2534Kahweol is one of the consituents of the coffeefrom Coffea Arabica with anti-inflammatoryanti-angiogenic, and anti-cancerous activities.Kahweol inhibits a

58、dipogenesis and increase glucoseuptake by AMP-activated protein kinase (AMPK)activation. Kahweol induces apoptosis.Karanjin is a major active furanoflavonolconstituent of Fordia cauliflora. Karanjin inducesGLUT4 translocation in skeletal muscle cells byincreasing AMPK activity. Karanjin can induceca

59、ncer cell death through cell cycle arrest andenhance apoptosis.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/kazinol-b.html Kazinol HYPERLINK https:/www.MedChemE/kazinol-b.ht

60、ml HYPERLINK https:/www.MedChemE/kazinol-b.html B HYPERLINK https:/www.MedChemE/kazinol-b.html HYPERLINK https:/www.MedChemE/kazinol-u.html Kazinol HYPERLINK https:/www.MedChemE/kazinol-u.html HYPERLINK https:/www.MedChemE/kazinol-u.html UCat. No.: HY-N3426 Cat. No.: HY-N3425Kazinol B, a prenylated