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
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 nar...
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-gl...
T2657	Elacridar	Elacridar (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.
T2893	Muscone	Muscone is an organic compound that is the primary contributor to the odor of musk.
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 adj...
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 a...
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 a...
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)...
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-gl...
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 p...
T6018	Zosuquidar 3HCl	Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
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.
T8426	Encequidar	Encequidar is a potent and selective P-glycoprotein inhibitor.
TMA2270	Alisol F 24-acetate	Alisol F 24-acetate is a natural product from Alisma plantago-aquatica Linn.
TN1023	Miltirone	Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.
TN1039	Tamarixetin	Tamarixetin has vasodilator effects in rat isolated vessels. Tamarixetin has cytotoxic against leukemia cells and in particular P-glycoprotein- overexpressing K...
TN1048	Cnidilin	Cnidilin has high BBB permeability and has pharmacokinetic potentials for the treatment of central nervous system diseases.
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...
TN1099	Dihydroevocarpine	Dihydroevocarpine shows potent anti-Helicobacter pylori activity with the minimum inhibitory concentration (MIC) value of 10-20 microg/ml. Dihydroevocarpine is ...
TN1421	Bacopaside II	Bacopaside II is a potential anti-angiogenic agent, it can reduce endothelial cell migration and tubulogenesis and induce apoptosis.
TN1425	Bacoside A3	Bacoside A3 has antioxidant potential, it shows comparatively higher neuroprotective response analysed as higher cell viability and decreased intracellular ROS.
TN1580	Dihydrodaidzein	Dihydrodaidzein-producing bacteria might lead to clarification of some of the mechanisms regulating the production of equol by fecal microbiota.
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 cong...
TN1757	Hypophyllanthin	Hypophyllanthin and phyllanthin have antitumour effects against Ehrlich Ascites Carcinoma in mice.
TN2233	Spathulenol	Spathulenol has immunomodulatory effect. Spathulenol shows the capacity to inhibit proliferation in the lymphocytes and to induce apoptosis in these cells possi...
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...
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 ...
TN2263	Tenacigenin B	Standard reference
TN2554	1-Monopalmitin	1-Monopalmitin has dielectric properties. 1-Monopalmitin inhibits the P-glycoprotein activity in intestinal Caco-2 cells.
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-T...
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-fe...
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 lym...
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...
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. <br/> 2. La...
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 daun...
TN4761	Phellamurin	Phellamurin inhibits intestinal P-glycoprotein in a dose-dependent manner, there is a serious interaction occurred between Phellamurin with cyclosporin, to ensu...
TN4819	(-)-Praeruptorin A	(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings depe...
TN5114	Taxinine	Taxinine and Taxinine B can inhibit the drug transport by P-glycoprotein in multidrug-resistant cells.
TN5118	Taxol C	1. Taxol C can reduce interaction with the P-glycoprotein transporter that may allow for increased permeation of taxanes into the brain. <br/>
TN5124	Taxuspine X	Taxuspine X may have p-glycoprotein inhibitory activity.
TQ0043	Dofequidar	Dofequidar (MS-209) is a quinoline compound that can reverse P-glycoprotein (P-gp)-mediated MDR.