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Membrane transporter/Ion channel P-gp

P-gp

P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1) or cluster of differentiation 243 (CD243) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. It exists in animals, fungi, and bacteria, and it likely evolved as a defense mechanism against harmful substances.P-gp is a glycoprotein that in humans is encoded by the ABCB1 gene. P-gp is a well-characterized ABC-transporter (which transports a wide variety of substrates across extra- and intracellular membranes) of the MDR/TAP subfamily. The normal excretion of xenobiotics back into the gut lumen by P-gp pharmacokinetically reduces the efficacy of some pharmaceutical drugs (which are said to be P-gp substrates). In addition, some cancer cells also express large amounts of P-gp, further amplifying that effect and rendering these cancers multidrug resistant.
Cat No. product name
T9173 HM-30181 mesylate monohydrate HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs.
T2S0410 Euphorbia factor L1 1. Euphorbia factor L1 can enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. 2. Euphorbia factor L1 inhibits the efflux of ABCB1 in KBv200 an...
TN1610 Epimagnolin A Epimagnolin A is a lignan obtained from the flower buds of Magnolia fargesii, which is traditionally used in Asian medicine for treating headache and nasal conge...
TN1425 Bacoside A3 Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.
TN1099 Dihydroevocarpine Dihydroevocarpine shows potent anti-Helicobacter pylori activity with the minimum inhibitory concentration (MIC) value of 10-20 microg/ml. Dihydroevocarpine is a...
TN1072 Lappaol A Lappaol A has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol A also ...
TN1048 Cnidilin Cnidilin has high BBB permeability and has pharmacokinetic potentials for the treatment of central nervous system diseases.
TQ0043 Dofequidar Dofequidar (MS-209) is a quinoline compound that can reverse P-glycoprotein (P-gp)-mediated MDR.
T3868 Agnuside Agnuside inhibits COX-2 (IC50: 0.026 mg/ml) but exhibits less than 10% inhibition of COX-1 at this concentration. It also inhibits 46.3, 66.8, and 82.1% of P-gly...
T2S0410 Euphorbia factor L1 1. Euphorbia factor L1 can enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. 2. Euphorbia factor L1 inhibits the efflux of ABCB1 in KBv200 an...
TN2254 Taccalonolide A Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is ...
T2S2018 7-beta-Hydroxylathyrol 7β-Hydroxylathyrol is a diterpenoid extract from the seed oil of Caper Spurge and displays P-gp inhibition resulting in cytotoxic properties.
T3002 Piperine Piperine (1-Piperoylpiperidine), a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
T3392 Sinapine thiocyanate Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800)....
T2893 Muscone Muscone is an organic compound that is the primary contributor to the odor of musk.
T6287 Tariquidar Tariquidar(Kd=5.1 nM) is a specific and effective non-competitive inhibitor of P-glycoprotein. It can reverse drug resistance in MDR cell Lines.
T6018 Zosuquidar 3HCl Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
T2657 Elacridar Elacridar (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.
TN2233 Spathulenol Spathulenol has immunomodulatory effect. Spathulenol shows the capacity to inhibit proliferation in the lymphocytes and to induce apoptosis in these cells possib...
TN2257 Tanshinone IIB Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a...
TN5124 Taxuspine X Taxuspine X may have p-glycoprotein inhibitory activity.
TN3937 Ent-16alpha,17-Dihydroxyatisan-3-one ent-16alpha,17-Dihydroxyatisan-3-one and ent-16alpha,17-dihydroxykauran-3-one have apoptosis induction activities on L5178 human MDR1 gene-transfected mouse lymp...
TN5118 Taxol C Taxol C can reduce interaction with the P-glycoprotein transporter that may allow for increased permeation of taxanes into the brain.
TN5114 Taxinine Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.
TN4819 (-)-Praeruptorin A (-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings depen...
TN4761 Phellamurin Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensur...
TN4749 Pepluanin A Pepluanin A, shows a very high activity for a jatrophane diterpene, outperforming cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated dauno...
TN4411 Lappaol F 1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade.
2. Lap...
TN4410 Lappaol C Lappaol C has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol C also ...
TN2727 Jatrophane 2 2,5,7,8,9,14-Hexaacetoxy-3-benzoyloxy-15-hydroxyjatropha-6(17),11E-diene (Jatrophane 2 ) exhibits significant antifeedant activity against a generalist plant-fee...
TN2263 Tenacigenin B Standard reference
TN2726 Jatrophane 5 Jatrophane 5 demonstrates the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-Tx...
TN2554 1-Monopalmitin 1-Monopalmitin has dielectric properties. 1-Monopalmitin inhibits the P-glycoprotein activity in intestinal Caco-2 cells.
TMA2270 Alisol F 24-acetate Alisol F 24-acetate is a natural product from Alisma plantago-aquatica Linn.
T4A2399 Cinobufotalin Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide pr...
T2A2486 5,7,3',4',5'-Pentamethoxyflavone 3',4',5',5,7-Pentamethoxyflavone has anti-inflammatory and cancer chemopreventive activities. 3',4',5',5,7-Pentamethoxyflavone could be used as an effective adju...
T16339 Norverapamil hydrochloride Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-gly...
T8426 Encequidar Encequidar is a potent and selective P-glycoprotein inhibitor.
T0012 Cinchonine Cinchonine, a local anesthetic of the amide type, now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local narc...
HM-30181 mesylate monohydrate
T9173CAS 2097125-58-9
HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs.
Euphorbia factor L1
T2S0410CAS 76376-43-7
1. Euphorbia factor L1 can enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. 2. Euphorbia factor L1 inhibits the efflux of ABCB1 in KBv200 an...
Epimagnolin A
TN1610CAS 41689-51-4
Epimagnolin A is a lignan obtained from the flower buds of Magnolia fargesii, which is traditionally used in Asian medicine for treating headache and nasal conge...
Bacoside A3
TN1425CAS 157408-08-7
Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.
Dihydroevocarpine
TN1099CAS 15266-35-0
Dihydroevocarpine shows potent anti-Helicobacter pylori activity with the minimum inhibitory concentration (MIC) value of 10-20 microg/ml. Dihydroevocarpine is a...
Lappaol A
TN1072CAS 62333-08-8
Lappaol A has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol A also ...
Cnidilin
TN1048CAS 14348-22-2
Cnidilin has high BBB permeability and has pharmacokinetic potentials for the treatment of central nervous system diseases.
Dofequidar
TQ0043CAS 129716-58-1
Dofequidar (MS-209) is a quinoline compound that can reverse P-glycoprotein (P-gp)-mediated MDR.
Agnuside
T3868CAS 11027-63-7
Agnuside inhibits COX-2 (IC50: 0.026 mg/ml) but exhibits less than 10% inhibition of COX-1 at this concentration. It also inhibits 46.3, 66.8, and 82.1% of P-gly...
Euphorbia factor L1
T2S0410CAS 76376-43-7
1. Euphorbia factor L1 can enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. 2. Euphorbia factor L1 inhibits the efflux of ABCB1 in KBv200 an...
Taccalonolide A
TN2254CAS 108885-68-3
Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is ...
7-beta-Hydroxylathyrol
T2S2018CAS 34208-98-5
7β-Hydroxylathyrol is a diterpenoid extract from the seed oil of Caper Spurge and displays P-gp inhibition resulting in cytotoxic properties.
Piperine
T3002CAS 94-62-2
Piperine (1-Piperoylpiperidine), a alkaloid, has been used in trials studying the treatment of multiple myeloma and deglutition disorders.
Sinapine thiocyanate
T3392CAS 7431-77-8
Sinapine Thiocyanate, is a derivative of Sinapine (S486605), an alkaloidal amine found in black mustard seeds. It is the choline ester of Sinapic Acid (S486800)....
Muscone
T2893CAS 541-91-3
Muscone is an organic compound that is the primary contributor to the odor of musk.
Tariquidar
T6287CAS 206873-63-4
Tariquidar(Kd=5.1 nM) is a specific and effective non-competitive inhibitor of P-glycoprotein. It can reverse drug resistance in MDR cell Lines.
Zosuquidar 3HCl
T6018CAS 167465-36-3
Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
Elacridar
T2657CAS 143664-11-3
Elacridar (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.
Spathulenol
TN2233CAS 6750-60-3
Spathulenol has immunomodulatory effect. Spathulenol shows the capacity to inhibit proliferation in the lymphocytes and to induce apoptosis in these cells possib...
Tanshinone IIB
TN2257CAS 17397-93-2
Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a...
Taxuspine X
TN5124CAS 194782-02-0
Taxuspine X may have p-glycoprotein inhibitory activity.
ent-16alpha,17-Dihydroxyatisan-3-one
TN3937CAS 112523-91-8
ent-16alpha,17-Dihydroxyatisan-3-one and ent-16alpha,17-dihydroxykauran-3-one have apoptosis induction activities on L5178 human MDR1 gene-transfected mouse lymp...
Taxol C
TN5118CAS 153415-45-3
Taxol C can reduce interaction with the P-glycoprotein transporter that may allow for increased permeation of taxanes into the brain.
Taxinine
TN5114CAS 3835-52-7
Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.
(-)-Praeruptorin A
TN4819CAS 14017-71-1
(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings depen...
Phellamurin
TN4761CAS 52589-11-4
Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensur...
Pepluanin A
TN4749CAS 670257-89-3
Pepluanin A, shows a very high activity for a jatrophane diterpene, outperforming cyclosporin A by a factor of at least 2 in the inhibition of Pgp-mediated dauno...
Lappaol F
TN4411CAS 69394-17-8
1. Lappaol F has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade.
2. Lap...
Lappaol C
TN4410CAS 64855-00-1
Lappaol C has antioxidant and antiaging properties, it may promote the C. elegans longevity and stress resistance through a JNK-1-DAF-16 cascade. Lappaol C also ...
Jatrophane 2
TN2727CAS 210108-86-4
2,5,7,8,9,14-Hexaacetoxy-3-benzoyloxy-15-hydroxyjatropha-6(17),11E-diene (Jatrophane 2 ) exhibits significant antifeedant activity against a generalist plant-fee...
Tenacigenin B
TN2263CAS 80508-42-5
Standard reference
Jatrophane 5
TN2726CAS 210108-89-7
Jatrophane 5 demonstrates the most powerful inhibition of P-gp, higher than R(+)-verapamil and tariquidar in colorectal multi-drug resistant (MDR) cells (DLD1-Tx...
1-Monopalmitin
TN2554CAS 542-44-9
1-Monopalmitin has dielectric properties. 1-Monopalmitin inhibits the P-glycoprotein activity in intestinal Caco-2 cells.
Alisol F 24-acetate
TMA2270CAS 443683-76-9
Alisol F 24-acetate is a natural product from Alisma plantago-aquatica Linn.
Cinobufotalin
T4A2399CAS 1108-68-5
Cinobufotalin is a main cardiac toxin in toad, it is a novel anti-HCC agent, it induces growth inhibition and apoptosis in cultured HCC cells through ceramide pr...
5,7,3',4',5'-Pentamethoxyflavone
T2A2486CAS 53350-26-8
3',4',5',5,7-Pentamethoxyflavone has anti-inflammatory and cancer chemopreventive activities. 3',4',5',5,7-Pentamethoxyflavone could be used as an effective adju...
Norverapamil hydrochloride
T16339CAS 67812-42-4
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-gly...
Encequidar
T8426CAS 849675-66-7
Encequidar is a potent and selective P-glycoprotein inhibitor.
Cinchonine
T0012CAS 118-10-5
Cinchonine, a local anesthetic of the amide type, now generally used for surface anesthesia. It is one of the most potent and toxic of the long-acting local narc...