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.

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.

A22637

CAS No.

57460-41-0

Talinolol

Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

Cat. No.

A25961

CAS No.

3371-85-5

Voacamine

Voacamine is an indole alkaloid that acts as an antagonist of the cannabinoid receptor 1 (CB1) and also functions as a P-glycoprotein (P-gp) inhibitor. This compound enhances the efficacy of Doxorubicin by modulating P-gp activity, promoting apoptosis-independent autophagic cell death in human osteosarcoma cells. Additionally, Voacamine activates mitochondrial-associated apoptosis signaling pathways while inhibiting the PI3K/Akt/mTOR pathway, thus suppressing breast cancer progression. Moreover, it demonstrates oncogenic activity against colorectal cancer by inhibiting epidermal growth factor receptor (EGFR).

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.

A59538

CAS No.

780750-65-4

AZD-5672

AZD-5672 is a potent and selective antagonist of the CCR5 receptor, exhibiting an IC50 of 0.32 nM. This compound demonstrates moderate activity against the hERG ion channel with a binding IC50 of 7.3 μM and acts as a substrate for human P-glycoprotein, inhibiting P-gp-mediated digoxin transport with an IC50 of 32 μM. AZD-5672 is an effective tool for investigating the role of CCR5 in inflammatory diseases, including rheumatoid arthritis.

Cat. No.

A62486

CAS No.

1169982-72-2

ORL1 antagonist 2

ORL1 antagonist 2 is a selective antagonist of the opioid receptor-like 1 (ORL1). This compound has been primarily utilized in the study of P-glycoprotein (P-gp) interactions and transport mechanisms. Its ability to modulate ORL1 activity makes it a valuable tool in research aimed at understanding opioid signaling pathways and their implications in various physiological and pathological processes.

Cat. No.

A67156

CAS No.

57982-78-2

Budipine

Budipine is an anti-Parkinson agent that acts primarily as an N-methyl-D-aspartate (NMDA) antagonist while also influencing dopaminergic activity. It enhances dopamine release and inhibits monoamine oxidase type B (MAO-B), contributing to its therapeutic effects. As a substrate of P-glycoprotein (P-gp), Budipine's uptake into the brain is mediated by this transport mechanism. This compound is valuable for research into central nervous system disorders, including Parkinson's disease.

Cat. No.

A67428

CAS No.

63661-61-0

Budipine hydrochloride

Budipine hydrochloride functions primarily as an anti-Parkinson agent, targeting the central nervous system. It acts as a substrate of P-glycoprotein (P-gp), facilitating its uptake into the brain. Additionally, Budipine hydrochloride serves as an NMDA antagonist and exhibits indirect dopaminergic effects by enhancing dopamine release and inhibiting monoamine oxidase type B (MAO-B). This compound is valuable for research focused on CNS disorders, particularly Parkinson's disease.

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.

A67819

CAS No.

477953-07-4

Neostenine

Synonyms: (+)-Neostenine

Neostenine is a stenine-type Stemona alkaloid that acts as a substrate for P-glycoprotein. It exhibits notable antitussive activity and demonstrates high absorptive permeability in Caco-2 monolayer models. Additionally, Neostenine shows oral bioactivity, making it relevant for research applications involving intestinal absorption and therapeutic potential in cough-related conditions.

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.

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.