P-glycoprotein-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html P-glycoproteinP-gp; Pgp; Multidrug resistance protein 1; MDR1; ATP-binding cassette sub-family B member 1; ABCB1;Cluster of differentiation 243; CD243P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important p

2、rotein of the cell membrane thatpumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity.P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) backinto the

3、intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where itpumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the bloodbrain barrier and blood-testisbarrier, where it pumps them back into the

4、 capillaries. Some cancer cells also express large amounts of P-gp, which renders thesecancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substratespecificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and

5、often mediates the development ofresistance to anticancer drugs. This protein also functions as a transporter in the bloodbrain barrier.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html P-glycoprotein HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html HYPERLINK https:/w

6、ww.MedChemE/Targets/P-glycoprotein.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html Agonists, HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html Activa

7、tors HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html & HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html HYPERLINK https:/www.MedChemE/Targets/P-glycoprotein.html Modulators HYPERLINK https:/www.MedChemE/_20S_-Protopanaxadio

8、l.html (20S)-Protopanaxadiol(20-Epiprotopanaxadiol; 20(S)-APPD) Cat. No.: HY-N0797 HYPERLINK https:/www.MedChemE/r-verapamil-d7-hydrochloride.html (R)-Verapamil HYPERLINK https:/www.MedChemE/r-verapamil-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/r-verapamil-d7-hydrochloride.html D7 HYPERLIN

9、K https:/www.MedChemE/r-verapamil-d7-hydrochloride.html HYPERLINK https:/www.MedChemE/r-verapamil-d7-hydrochloride.html hydrochloride(R)-(+)-Verapamil D7 hydrochloride) Cat. No.: HY-135336S20S-protopanaxadiol (aPPD) is a metabolite ofginseng saponins, inhibits Akt activity andinduces apoptosis in va

10、rious tumor cells.(R)-Verapamil D7 hydrochloride (R)-(+)-VerapamilD7 hydrochloride) is a deuterium labeled(R)-Verapamil hydrochloride. (R)-Verapamilhydrochloride (R)-(+)-Verapamil hydrochloride) isa P-Glycoprotein inhibitor.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg,

11、50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/r-verapamil-hydrochloride.html (R)-Verapamil HYPERLINK https:/www.MedChemE/r-verapamil-hydrochloride.html HYPERLINK https:/www.MedChemE/r-verapamil-hydrochloride.html hydrochloride(R)-(+)-Verapamil hydroch

12、loride) Cat. No.: HY-135336 HYPERLINK https:/www.MedChemE/atazanavir.html Atazanavir(BMS-232632) Cat. No.: HY-17367(R)-Verapamil hydrochloride (R)-(+)-Verapamilhydrochloride) is a P-Glycoprotein inhibitor.(R)-Verapamil hydrochloride blocks MRP1 mediatedtransport, resulting in chemosensitization ofMR

13、P1-overexpressing cells to anticancer drugs.Atazanavir (BMS-232632), a highly selective HIV-1protease inhibitor, is the first proteaseinhibitor approved for once-daily administration.Atazanavir (BMS-232632) is a substrate andinhibitor of CYP3A4, and an inhibitor and inducerof P-glycoprotein (P-gp).P

14、urity: 98.54%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.html Atazanavir HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.html HYPERLINK https:/www.MedChemE/Atazanavir-sulfate.h

15、tml sulfate(BMS-232632 sulfate) Cat. No.: HY-17367A HYPERLINK https:/www.MedChemE/atazanavir-d5.html Atazanavir-d5Cat. No.: HY-17367S3Atazanavir (BMS-232632) sulfate, a highlyselective HIV-1 protease inhibitor, is the firstprotease inhibitor approved for once-dailyadministration. Atazanavir sulfate

16、is a substrateand inhibitor of CYP3A4, and an inhibitor andinducer of P-glycoprotein (P-gp).Atazanavir-d5 is the deuterium labeled Atazanavir.Atazanavir (BMS-232632), a highly selective HIV-1protease inhibitor, is the first proteaseinhibitor approved for once-daily administration.Purity: 99.94%Clini

17、cal Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mg HYPERLINK https:/www.MedChemE/atazanavir-d6.html Atazanavir-d6 HYPERLINK https:/www.MedChemE/atazanavir-d6.html HYPERLINK https:/www.MedChemE/atazanavir-d9.html Atazanavir-d9(BM

18、S-232632-d6) Cat. No.: HY-17367S4 (BMS-232632-d9) Cat. No.: HY-17367S2Atazanavir-d6 is deuterium labeled Atazanavir.Atazanavir (BMS-232632), a highly selective HIV-1protease inhibitor, is the first proteaseinhibitor approved for once-daily administration.Atazanavir-d9 (BMS-232632-d9) is the deuteriu

19、mlabeled Atazanavir. Atazanavir (BMS-232632), ahighly selective HIV-1 protease inhibitor, is thefirst protease inhibitor approved for once-dailyadministration.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYP

20、ERLINK https:/www.MedChemE/azd-5672.html AZD-5672 HYPERLINK https:/www.MedChemE/azd-5672.html HYPERLINK https:/www.MedChemE/Biricodar.html BiricodarCat. No.: HY-119101(VX-710) Cat. No.: HY-13574AAZD-5672 is an orally active, potent, andselective CCR5 antagonist (IC =0.32 nM).50AZD-5672 shows moderat

21、e activity against the hERGion channel (binding IC =7.3 M).50Biricodar (VX-710) is a modulator of P-glycoproteinand MRP-1; shows effective chemosensitizingactivity in multidrug resistant cells.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical

22、 Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/boeravinone-b.html Boeravinone HYPERLINK https:/www.MedChemE/boeravinone-b.html HYPERLINK https:/www.MedChemE/boeravinone-b.html B HYPERLINK https:/www.MedChemE/boer

23、avinone-b.html HYPERLINK https:/www.MedChemE/chrysosplenetin.html ChrysosplenetinCat. No.: HY-N2947 Cat. No.: HY-N1457Boeravinone B, a dual inhibitor of NorA bacterialefflux pump of Staphylococcus aureus and humanP-Glycoprotein, reduces the biofilm formation andintracellular invasion of bacteria. Bo

24、eravinone Bact as anti-aging and anti-apoptosisphyto-molecules during oxidative stress.Chrysosplenetin is one of the polymethoxylatedflavonoids in Artemisia annua L. (Compositae)and other several Chinese herbs. Chrysosplenetininhibits P-gp activity and reverses theup-regulated P-gp and MDR1 levels i

25、nduced byartemisinin (ART).Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.52%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mg HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html Coniferyl HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html HYPER

26、LINK https:/www.MedChemE/coniferyl-ferulate.html ferulate HYPERLINK https:/www.MedChemE/coniferyl-ferulate.html HYPERLINK https:/www.MedChemE/convallatoxin.html ConvallatoxinCat. No.: HY-N1916 Cat. No.: HY-N2453Coniferyl ferulate, a strong inhibitor ofglutathione S-transferase (GST), reversesmultidr

27、ug resistance and downregulatesP-glycoprotein. Coniferyl ferulate shows stronginhibition of human placental GST with an IC of500.3M.Convallatoxin is a cardiac glycoside isolated fromAdonis amurensis Regel et Radde. Convallatoxinameliorates colitic inflammation via activation ofPPAR and suppression o

28、f NF-B.Purity: 98.56%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98.66%Clinical Data: No Development ReportedSize: 5 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html CP-100356 HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html HYPERLINK htt

29、ps:/www.MedChemE/cp-100356-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html HYPERLINK https:/www.MedChemE/Dofequidar.html DofequidarCat. No.: HY-108347 Cat. No.: HY-17013CP-100356 hydrochloride is an orally active dualMDR1 (P-gp)/BCRP inhibitor, with an IC

30、s of500.5 and 1.5 M for inhibiting MDR1-mediatedCalcein-AM transport and BCRP-mediated Prazosintransport, respectively.Dofequidar(MS-209) is a novel quinoline compound,which can reverse P-glycoprotein (P-gp)-mediatedMDR.Purity: 99.68%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50

31、 mgPurity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Dofequidar-fumarate.html Dofequidar HYPERLINK https:/www.MedChemE/Dofequidar-fumarate.html HYPERLINK https:/www.MedChemE/Dofequidar-fumarate.html fumarate HYPERLINK https:/www.MedChemE/Dofequidar-fumarate.html HYPERLI

32、NK https:/www.MedChemE/elacridar.html Elacridar(MS-209) Cat. No.: HY-17013A (GF120918; GW0918; GG918; GW120918) Cat. No.: HY-50879Dofequidar fumarate(MS-209 fumarate), an orallyactive quinoline compound, has been reported toovercome MDR by inhibiting ABCB1/P-gp,ABCC1/MDR-associated protein 1, or bot

33、h.Elacridar (GF120918) is a potent P-glycoprotein(Pgp) and BCRP inhibitor.Purity: 98.40%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.80%Clinical Data: No Development ReportedSize: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/elacridar-hydrochlori

34、de.html Elacridar HYPERLINK https:/www.MedChemE/elacridar-hydrochloride.html HYPERLINK https:/www.MedChemE/elacridar-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/elacridar-hydrochloride.html HYPERLINK https:/www.MedChemE/HM30181.html Encequidar(GF120918A) Cat. No.: HY-50880 (HM3018

35、1; HM30181A) Cat. No.: HY-13646Elacridar hydrochloride (GF120918A) is a potentP-glycoprotein (Pgp) and BCRP inhibitor.Encequidar (HM30181; HM30181A) is a potent andselective inhibitor of P-glycoprotein.Purity: 99.73%Clinical Data: No Development ReportedSize: 10 mg, 50 mg, 100 mgPurity: 98.0%Clinica

36、l Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/HM30181_mesylate.html Encequidar HYPERLINK https:/www.MedChemE/HM30181_mesylate.html HYPERLINK https:/www.MedChemE/HM30181_mesylate.html mesylate(HM30181 mesylate; HM30181A mesylate) Cat. No.: HY-13646A HYPER

37、LINK https:/www.MedChemE/epoxylathyrol.html EpoxylathyrolCat. No.: HY-N0425Encequidar mesylate (HM30181 mesylate; HM30181Amesylate) is a competitive and potentP-glycoprotein inhibitor.Epoxylathyrol, an epoxylathyrane derivativeisolated from the Euphorbia boetica, is aP-glycoprotein (P-gp) inhibitor.

38、 Epoxylathyrol isa P-gp-mediated multidrug resistance (MDR)reverser.Purity: 99.90%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/evodine.html EvodineCat. No.: HY-N0689 HYPERLINK

39、 https:/www.MedChemE/fd-12-9.html FD HYPERLINK https:/www.MedChemE/fd-12-9.html HYPERLINK https:/www.MedChemE/fd-12-9.html 12-9(Ac12Az9) Cat. No.: HY-128685Evodine, the major limonoid of Evodiae Fuctus, isa potent P-gp inhibitor. Evodine has protectionagainst glutamateinduced toxicity by preservingt

40、he antioxidant defense system.FD 12-9 is a flavonoid dimer, acts as a dualinhibitor of P-gp and BCRP, with EC s of 28550nM and 0.9 nM, respectively. Anti-glioblastomaactivity.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 98%Clinical Data: No Development ReportedSiz

41、e: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/furanodiene.html FuranodieneCat. No.: HY-126940 HYPERLINK https:/www.MedChemE/glibenclamide.html Glibenclamide(Glyburide) Cat. No.: HY-15206Furanodiene is a natural terpenoid isolated fromRhizoma Curcumae. Furanodiene playsanti-cancer effects through anti-

42、angiogenesis andinducing ROS production, DNA strand breaks andapoptosis.Glibenclamide (Glyburide) is an orally activeATP-sensitive K+ channel (K ) inhibitor andATPcan be used for the research of diabetes andobesity. Glibenclamide inhibits P-glycoprotein.Purity: 98%Clinical Data: No Development Repor

43、tedSize: 5 mg, 10 mg, 25 mgPurity: 99.79%Clinical Data: LaunchedSize: 10 mM 1 mL, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/glyburide-d11.html Glyburide-d11 HYPERLINK https:/www.MedChemE/glyburide-d11.html HYPERLINK https:/www.MedChemE/glyburide-d3.html Glyburide-d3Cat. No.: HY-15206S(Glyburide

44、-d3) Cat. No.: HY-15206S1Glyburide-d11 is the deuterium labeledGlibenclamide. Glibenclamide (Glyburide) is anorally active ATP-sensitive K+ channel (K )ATPinhibitor and can be used for the research ofdiabetes and obesity. Glibenclamide inhibitsP-glycoprotein.Glyburide-d3 (Glyburide-d3) is the deuter

45、iumlabeled Glibenclamide. Glibenclamide (Glyburide)is an orally active ATP-sensitive K+ channel(K ) inhibitor and can be used for theATPresearch of diabetes and obesity. Glibenclamideinhibits P-glycoprotein.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 10 mgPurity: 98%Clinical Data: N

46、o Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/htt-d3.html HTT-D3 HYPERLINK https:/www.MedChemE/htt-d3.html HYPERLINK https:/www.MedChemE/hypophyllanthin.html HypophyllanthinCat. No.: HY-143792 Cat. No.: HY-N4108HTT-D3 is a potent and orally active huntingtin(HTT) splicing modu

47、lator. HTT-D3 acts bypromoting the inclusion of a pseudoexon containinga premature termination codon (stop-codonpsiExon), leading to HTT mRNA degradation andreduction of HTT levels.Hypophyllanthin is a major lignan in Phyllanthusspp, with strong anti-inflammatory activity.Hypophyllanthin directly in

48、hibits P-glycoprotein(P-gp) activity and did not interfere withmultidrug resistance protein 2 (MRP2) activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChem

49、E HYPERLINK https:/www.MedChemE/isosinensetin.html IsosinensetinCat. No.: HY-N1941 HYPERLINK https:/www.MedChemE/laniquidar.html Laniquidar(R101933) Cat. No.: HY-132189Isosinensetin, a polymethoxylated flavoneextracted from pericarpium citri reticulataeviride, exhibits inhibition on P-glycoprotein(P

50、-gp) in MDR1-MDCKII cells.Laniquidar (R101933) is a noncompetitive, thirdgeneration P-glycoprotein (P-gp) inhibitor with anIC of 0.51 M. Laniquidar can be used for50modulating multidrug resistance transporters.Purity: 99.26%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 98%Cli

51、nical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/mc70.html MC70 HYPERLINK https:/www.MedChemE/mc70.html HYPERLINK https:/www.MedChemE/MCI826.html MCI826Cat. No.: HY-113805 Cat. No.: HY-U00247MC70 is a potent and non-selective P-glycoprotein(P-gp) inhibitor with an EC

52、 of 0.69 M. MC7050is an ABC transporters inhibitor and anticanceragent. MC70 interacts with ABCB1, ABCG2 and ABCC1.MCI826 is a P-glycoprotein (P-gp) antagonist.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK

53、 https:/www.MedChemE/norverapamil.html Norverapamil()-Norverapamil; D591) Cat. No.: HY-135328 HYPERLINK https:/www.MedChemE/Norverapamil-hydrochloride.html Norverapamil HYPERLINK https:/www.MedChemE/Norverapamil-hydrochloride.html HYPERLINK https:/www.MedChemE/Norverapamil-hydrochloride.html hydroch

54、loride()-Norverapamil hydrochloride; D591 hydrochloride) Cat. No.: HY-100750Norverapamil ()-Norverapamil), an N-demethylatedmetabolite of Verapamil, is a L-type calciumchannel blocker and a P-glycoprotein (P-gp)function inhibitor.Norverapamil hydrochloride ()-Norverapamilhydrochloride), an N-demethy

55、lated metabolite ofVerapamil, is a L-type calcium channel blocker anda P-glycoprotein (P-gp) function inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.26%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChem

56、E/norverapamil-d7.html Norverapamil-d7 HYPERLINK https:/www.MedChemE/norverapamil-d7.html HYPERLINK https:/www.MedChemE/NSC23925.html NSC23925()-Norverapamil-d7; D591-d7) Cat. No.: HY-135328SCat. No.: HY-19626Norverapamil-d7 ()-Norverapamil-d7) is adeuterium labeled Norverapamil ()-Norverapamil).Nor

57、verapamil, an N-demethylated metabolite ofVerapamil, is a L-type calcium channel blocker anda P-glycoprotein (P-gp) function inhibitor.NSC23925 is a novel, selective and effectiveP-glycoprotein (Pgp) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.48%Clinical Da

58、ta: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/ont-093.html ONT-093 HYPERLINK https:/www.MedChemE/ont-093.html HYPERLINK https:/www.MedChemE/P-gp_inhibitor_1.html P-gp HYPERLINK https:/www.MedChemE/P-gp_inhibitor_1.html HYPERLINK https:/www.MedChemE/P-g

59、p_inhibitor_1.html inhibitor HYPERLINK https:/www.MedChemE/P-gp_inhibitor_1.html HYPERLINK https:/www.MedChemE/P-gp_inhibitor_1.html 1(OC 144-093; OC 144093) Cat. No.: HY-15134Cat. No.: HY-101791ONT-093 is a potent inhibitor of P-glycoproteinpump. ONT-093 has the potential for theresearch cancer dis

60、eases.P-gp inhibitor 1 is a novel inhibitor reversingP-glycoprotein-mediated multidrug resistance.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/p-gp-inhibitor-2.html P-gp