P-gp

P-gp

The crucial cell membrane protein known as P-glycoprotein (P-gp), also referred to as multidrug resistance protein 1 (MDR1), is responsible for expelling a variety of foreign substances. It is an ATP-dependent efflux pump with a broad substrate specificity, to put it more precisely. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood-brain barrier and blood-testis barrier, where it pumps them back into the capillaries.Additionally, some cancer cells overexpress P-gp, making these cancers multi-drug resistant. P-gp is a broad substrate specificity ATP-dependent drug efflux pump for xenobiotic compounds. It controls the reduced drug accumulation in cells with multiple drug resistance and frequently controls the emergence of anticancer drug resistance. The blood-brain barrier uses this protein as a transporter as well.

P-gp related products

Structure Cat No. Product Name CAS No. Product Description
V77720 ABCB1-IN-1 ABCB1-IN-1 (compound 3) is a potent inhibitor of ABCB1.
V79976 Anticancer agent 108 Anticancer agent 108 (Compound 3.10) is a potent P-gp inhibitor (antagonist) with anti-tumor activity and low toxicity to normal and pseudonormal cells.
V74216 Boeravinone B 114567-34-9 Boeravinone B is a dual (bifunctional) inhibitor of Staphylococcus aureus and human P-glycoprotein NorA bacterial efflux pumps, which can reduce bacterial biofilm formation and invasion.
V1296 Elacridar (GF120918) 143664-11-3 Elacridar (formerly GW-120918; GF-120918; GG-918;GW-0918;GF120918; GF120918; GW0918; GG918) is a 3rd generationl and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor that has the potential to overcome P-gp-mediated multidrug resistance (MDR) of the cytotoxic drugs such as doxorubicin.
V2620 Elacridar HCl (GF120918A) 143851-98-3 ElacridarHCl (formerly also known as GF120918; GF-120918; GW0918; GG918; GW120918) is a novel and potent P-glycoprotein (P-gp or MDR-1) and BCRP inhibitor.
V20530 Encequidar (HM-30181; HM-30181A) 849675-66-7 Encequidar (formerly HM-30181; HM30181; HM30181A) is a novel, potent, selective, and orally bioavailable inhibitor of the adenosine triphosphate (ATP)-binding cassette (ABC) transporter P-gp (P-glycoprotein).
V22218 Encequidar mesylate (HM-30181; HM-30181A) 849675-87-2 Encequidarmesylate (HM30181; HM-30181A; Oraxol), the mesylate salt of encequidar, is a novel,highly specific, andorally bioavailable inhibitor of P-glycoprotein (P-gp), which is an adenosine triphosphate (ATP)-binding cassette (ABC) transporter.
V74213 Encequidar mesylate hydrochloride (HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride) 2097125-58-9 Encequidar (HM30181) mesylate HCl is a potent and specific inhibitor of P-glycoprotein (MDR1).
V74221 Epoxylathyrol 28649-60-7 Epoxylathyrol is an epoxyethoxy ether analogue extracted from Euphorbia boetica.
V74224 Euphohelioscopin A 87064-61-7 Euphohelioscopin A is a diterpenoid that can be extracted from the Euphorbia helioscopia L.plant.
V74222 FM04 1807320-40-6 FM04 is a potent inhibitor of P-glycoprotein (P-gp) (EC50=83 nM).
V74219 Ganoderenic acid B 100665-41-6 Ganoderenic acid B is a triterpenoid extracted from Ganoderma lucidum.
V74226 Jatrophane 5 210108-89-7 Jatrophane 5 is a naturally occurring compound derived from Jatropha carcas L.
V74225 Neostenine ((+)-Neostenine) 477953-07-4 Neostenine is a statin-type alkaloid with antitussive activity.
V5031 NSC23925 HCl 858474-14-3 NSC23925 2HCl (NSC23925 dihyrochloride) is a novel, potent, selective and effective P-glycoprotein (Pgp) inhibitor that is able to reverse multidrug resistance (MDR), e.
V74217 OY-101 41183-02-2 OY-101 is an orally bioavailable and specific P-glycoprotein (P-gp) inhibitor.
V81106 P-gp inhibitor 13 P-gp inhibitor 13 is a P-gp inhibitor.
V74223 P-gp inhibitor 14 2892571-47-8 P-gp inhibitor 14 (Compound 8a) is a high-affinity P-gp inhibitor.
V81107 P-gp inhibitor 15 P-gp inhibitor 15 (compound 7a) is a non-substrate inhibitor of P-glycoprotein (Pgp).
V81108 P-gp/BCRP-IN-2 P-gp/BCRP-IN-2 (compound 15) is an oxadiazole analogue and a dual (bifunctional) inhibitor of the ABC transporter P-glycoprotein (IC50= 1.6 nM) and BCRP (IC50= 600 nM).
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