P-gp

Cat. No.

A11080

CAS No.

121584-18-7

Valspodar (PSC-833)

Synonyms: PSC833; Amdray

PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).

Cat. No.

A12249

CAS No.

67812-42-4

Norverapamil hydrochloride

Synonyms: (±)-Norverapamil hydrochloride; D591 hydrochloride

Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

Cat. No.

A12679

CAS No.

52-53-9

Verapamil

Synonyms: CP-16533-1; ±-Verapamil

Verapamil is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor.

Cat. No.

A13533

CAS No.

174254-13-8

Biricodar dicitrate (VX-710)

Synonyms: VX-710 dicitrate; VX-710

Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

Cat. No.

A15289

CAS No.

167354-41-8

Zosuquidar

Synonyms: LY335979

Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.

Cat. No.

A20054

CAS No.

2249749-39-9

P-gp modulator 1

P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).

Cat. No.

A21464

CAS No.

159997-94-1

Biricodar

Synonyms: VX-710

Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.

Cat. No.

A25165

CAS No.

293736-67-1

Berubicin hydrochloride

Synonyms: RTA 744; WP 744; WP 769 hydrochloride

Berubicin hydrochloride is an NF-kB agonist and a Doxorubicin analog with the ability to cross the blood-brain barrier. It inhibits P-glycoprotein (P-gp) and multidrug resistance-associated protein 1 (MRP1), thereby reducing efflux in glioblastoma multiforme (GBM) and exerting cytotoxic effects on leukemia cells. Additionally, Berubicin hydrochloride induces apoptosis in neuroblastoma cells, making it a valuable reagent for studying tumors of the nervous system.

Cat. No.

A34309

CAS No.

58735-64-1

Roquefortine C

Roquefortine C is a mycotoxin derived from Penicillium species, exhibiting multiple biological activities. As an agonist of P-glycoprotein (P-gp), it inhibits cytochrome P450 enzymes, specifically P450 3A and P450 1A. This compound demonstrates antimicrobial effects against Gram-positive bacteria and possesses neurotoxic properties, along with potential antitumor activity. Roquefortine C serves as a valuable tool in research exploring microbial interactions and pharmacological mechanisms.

Cat. No.

A53900

CAS No.

2487457-15-6

Anticancer agent 50

Anticancer agent 50 is a potent modulator of the ABCB1 efflux pump, demonstrating significant cytotoxic and antiproliferative effects. This compound effectively reduces cyclin D1 expression while inducing p53 expression, highlighting its role in cell cycle regulation. Anticancer agent 50 is particularly relevant for research focused on T-lymphoma and other cancers associated with ABCB1 activity.

Cat. No.

A66411

CAS No.

67018-85-3

Norverapamil

Synonyms: (±)-Norverapamil; D591

Norverapamil, an N-demethylated metabolite of Verapamil, acts as an L-type calcium channel blocker and inhibits P-glycoprotein (P-gp) function. This compound is primarily utilized in research to study calcium ion dynamics and assess the role of P-gp in drug transport and resistance mechanisms. Its ability to modulate calcium influx makes it valuable for applications in cardiovascular and neuropharmacological investigations.

Cat. No.

A67803

CAS No.

3112403-98-9

WS-917

WS-917 is a potent orally active modulator of the ATP-binding cassette transporter ABCB1. It enhances ABCB1 ATPase activity, thereby increasing the efficacy of chemotherapeutics such as paclitaxel, particularly in combination with anti-PD-1 antibodies. Additionally, WS-917 is known to promote the activation of CD8+ T-cells, making it a valuable tool for research in cancer immunotherapy and drug resistance studies.

Cat. No.

A67818

CAS No.

2035417-32-2

WS-691

WS-691 is a selective modulator of the ATP-binding cassette sub-family B member 1 (ABCB1). This compound directly binds to ABCB1, stabilizing its structure, which inhibits its efflux function and activates its ATPase activity. By elevating intracellular levels of Paclitaxel, WS-691 reduces the necessary dosage of this chemotherapeutic agent in cancer cells that overexpress ABCB1. It enhances the sensitivity of colon cancer cells to Paclitaxel, making it a valuable tool for studying drug resistance mechanisms and improving cancer treatment strategies.

Cat. No.

A67835

CAS No.

180422-22-4

XR9051 hydrochloride

XR9051 hydrochloride is a selective modulator of P-glycoprotein, acting specifically on its function to address multidrug resistance (MDR) in cancer cells. This compound enhances the efficacy of various chemotherapeutics by inhibiting the P-glycoprotein transport mechanism, thereby improving drug retention within resistant cell lines. XR9051 is utilized in research focused on overcoming drug resistance in oncology.

Cat. No.

A67839

CAS No.

2987145-05-9

P-gp modulator 2

P-gp Modulator 2 is a potent competitive allosteric modulator of P-glycoprotein (P-gp). This compound significantly influences drug transport and can enhance the bioavailability of various therapeutic agents by inhibiting P-gp-mediated efflux. Its applications in research include studying drug-drug interactions and understanding mechanisms of multidrug resistance in cancer.

Cat. No.

A67852

CAS No.

2987145-15-1

P-gp modulator 3

P-gp modulator 3 is a potent, competitive allosteric modulator of P-glycoprotein (P-gp). This compound enhances the effectiveness of therapeutic agents by inhibiting P-gp-mediated efflux, thus promoting improved intracellular accumulation of drugs. It is particularly useful in research applications focused on drug resistance mechanisms and the development of multi-drug resistance inhibitors.

Cat. No.

A67859

CAS No.

2652001-05-1

P-gp inhibitor 4

P-gp inhibitor 4 is a selective modulator of P-glycoprotein, exhibiting an EC50 of 94 nM. This compound enhances the transport of therapeutic agents across the gastrointestinal barrier and can restore the efficacy of doxorubicin in multidrug-resistant cancer cells. It serves as a valuable tool for research into overcoming drug resistance and improving drug delivery mechanisms.

Cat. No.

A67866

CAS No.

762219-35-2

XR9051

XR9051 is a specific modulator of P-glycoprotein, targeting multidrug resistance (MDR). This compound enhances the efficacy of chemotherapeutic agents by inhibiting P-glycoprotein activity, thereby improving drug accumulation in resistant cancer cells. XR9051 is primarily utilized in cancer research to investigate strategies for overcoming drug resistance and enhancing therapeutic outcomes.

Cat. No.

A67876

CAS No.

2220141-46-6

VU6007477

VU6007477 is a selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM, notable for its ability to penetrate the blood-brain barrier. This compound also acts as a human P-glycoprotein (P-gp) substrate and exhibits moderate permeability, providing advantages in central nervous system (CNS) research. As a pyranyl amide derivative, VU6007477 is a valuable tool for investigating cholinergic seizure activity and related neurological disorders.

Cat. No.

A67878

CAS No.

140646-80-6

MCI826

MCI826 is a P-glycoprotein (P-gp) agonist that enhances the efflux of various substrates across cell membranes. Its primary biological activity focuses on modulating drug transport and influencing cellular drug accumulation. This compound is valuable in research applications related to pharmacokinetics, multidrug resistance, and therapeutic strategies involving P-gp.

Cat. No.

B10912

CAS No.

2924484-79-5

(S)-OY-101

(S)-OY-101 is a stereoisomer of OY-101, primarily acting as a selective modulator of natural signaling pathways. This compound exhibits significant biological activity in the context of research applications related to cellular signaling and metabolic regulation. It serves as a valuable tool for studying the effects of stereochemistry on biological processes and has potential applications in drug discovery and development.