49 Results for "

Drug efflux

" in MedChemExpress (MCE) Product Catalog:
Products (49)

49 Results for "Drug efflux" in MCE Product Catalog:

2
2 Cited Publications
Cat. No.: HY-107643
CAS No.: 313397-13-6
Purity:  99.90%
Synonyms: CBLC4H10
Target:  

P-glycoprotein

Research Areas:  

Cancer

Reversan (CBLC4H10) inhibits drug efflux mediated by P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP1), and exhibits oral activity. Reversan shows activity against glioblastoma multiforme and neuroblastoma models .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-17013
CAS No.: 129716-58-1
Synonyms: MS-209 free base
Target:  

P-glycoprotein

Research Areas:  

Cancer

Dofequidar (MS-209 free base) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-137433
CAS No.: 1835667-63-4
Purity:  99.86%
Synonyms: D-0316
Research Areas:  

Cancer

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-17013A
CAS No.: 153653-30-6
Synonyms: MS-209
Target:  

P-glycoprotein

Research Areas:  

Cancer

Dofequidar fumarate (MS-209) is an orally active quinoline compoundthat blocks P-glycoprotein (P-gp) and multidrug resistance-associated protein-1 (MDR-1). Dofequidar fumarate has highly potent reversing effect on multidrug-resistant tumor cells. Dofequidar fumarate competitively inhibits ABCB1/P-gp, ABCC1/MRP-1, blocks the efflux of chemotherapeutic agents, increases the drug concentration in cancer cells, and enhances the chemotherapeutic effect .
loading...
    loading...
Cat. No.: HY-401424
CAS No.: 61791-12-6
Synonyms: Polyoxyethylene(36) Castor Oil; PEG-36 Castor Oil
Cremophor EL-36 is a non-ionic surfactant, mainly used as a solubilizing carrier for poorly soluble Paclitaxel (HY-B0015). For example, Cremophor EL-36 can enhance the intracellular influx of Etoposide (HY-13629) without affecting drug efflux, and can dose-dependently increase the accumulation of VP-16 in lung adenocarcinoma cells (such as PC-14 and A549), significantly enhancing its cytotoxic effect .
loading...
    loading...
Cat. No.: HY-D0180
CAS No.: 17455-13-9
Synonyms: 18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane
18-Crown-6-ether is a type of crown ether compound and a specific structure dissociating agent. 18-Crown-6-ether can compete with K + for binding to G-quadruplexes, disrupting their stable structure to regulate the functions of related systems. 18-Crown-6-ether combines with K + and other metal ions to achieve precise ion transmembrane transport. 18-Crown-6-ether can act as an "susceptibility substrate" for the multi-drug efflux pump EmrE (a bacterial multidrug resistance transporter), ultimately inhibiting bacterial growth. 18-Crown-6-ether can be used in microcapsule controlled release and the research on developing antibacterial enhancers .
loading...
    loading...
Cat. No.: HY-12758
CAS No.: 1346753-00-1
Purity:  99.16%
Target:  

BCRP

Research Areas:  

Cancer

YHO-13351 is an orally active ABCG2 inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer .
loading...
    loading...
Cat. No.: HY-15134
CAS No.: 216227-54-2
Purity:  99.21%
Synonyms: OC 144-093; OC 144093
Target:  

P-glycoprotein

Research Areas:  

Infection Cancer

ONT-093 (OC 144-093) is a potent and orally active inhibitor of P-glycoprotein pump. ONT-093 inhibits P-gp-mediated ATPase activity with an IC50 of 0.16 μM. ONT-093 can inhibit drug efflux and increase bioavailability. ONT-093 reverses cancer cells multidrug resistance to chemotherapeutic drugs. ONT-093 can be used for the researches of cancer and infection, such as colon cancer and malarial .
loading...
    loading...
Cat. No.: HY-B0501
CAS No.: 119478-55-6
Synonyms: CP 76136-27
Research Areas:  

Infection

Danofloxacin mesylate (CP 76136-27) is a fluoroquinolone used as a veterinary drug. Danofloxacin mesylate has a broad spectrum of bactericidal activity, mainly inhibiting the DNA cycloenzyme of the bacteria. In addition, Danofloxacin mesylate is a substrate for ATP-dependent efflux transporters (P-gp and MRP2) .
loading...
    loading...
Cat. No.: HY-144880
CAS No.: 1977557-86-0
Purity:  99.52%
Synonyms: 3-Aminophenyl Hemiasterlin
Research Areas:  

Cancer

SC209 (3-Aminophenyl Hemiasterlin) is a 3-aminophenyl hemiasterlin derivative that serves as a cytotoxin for ADCs, targeting tubulin. SC209 has reduced potential for drug efflux via P-glycoprotein 1 drug pump compared with other tubulin-targeting payloads. SC209 exhibits antitumor activity and can be used in the synthesis of ADC molecules .
loading...
    loading...
Cat. No.: HY-N0566
CAS No.: 85999-40-2
Synonyms: Anemosapogenin
23-Hydroxybetulinic acid (Anemosapogenin) is an orally active triterpenoid with broad-spectrum anticancer activity. 23-Hydroxybetulinic acid reduces the levels of Bcl-2 and survivin, elevates the level of Bax, promotes the cleavage/activation of caspase-3 and caspase-9, and induces apoptosis via the endogenous mitochondrial pathway involving cytochrome C release and mitochondrial membrane potential disruption. 23-Hydroxybetulinic acid arrests the cell cycle at S and G1 phases, inhibits cancer cell proliferation, blocks the MAPK signaling pathway, regulates MMP2, and induces autophagic apoptosis by upregulating beclin-1. 23-Hydroxybetulinic acid inhibits the activity and efflux function of P-gp, increases the intracellular accumulation of chemotherapeutic drugs, and synergistically enhances cytotoxicity with Doxorubicin (HY-15142). 23-Hydroxybetulinic acid inhibits the phosphorylation and nuclear translocation of STAT6, blocks M2 macrophage polarization, and reduces M2 macrophage-mediated apoptosis resistance of colon cancer cells. 23-Hydroxybetulinic acid can be used in related studies on chronic myeloid leukemia, hepatocellular carcinoma, sarcoma 180, multidrug-resistant breast cancer, leukemia, Doxorubicin-induced cardiotoxicity, and colorectal cancer .
loading...
    loading...
Cat. No.: HY-145301
CAS No.: 65840-95-1
Target:  

Bacterial

Research Areas:  

Infection

Mycobactin-IN-1, a pyrazoline analogue, is a mycobactin biosynthesis inhibitor against mycobacteria. Mycobactin-IN-1 binds to salicyl-AMP ligase (MbtA), a key enzyme in the mycobactin biosynthetic pathway. Mycobactin-IN-1 inhibits whole-cell drug efflux pumps in M. smegmatis. Mycobactin-IN-1 eradicates intracellularly surviving mycobacteria. Mycobactin-IN-1 shows an excellent in vivo pharmacokinetic profile. Mycobactin-IN-1 can be used for the research of tuberculosis .
loading...
    loading...
Cat. No.: HY-173162
CAS No.: 86383-89-3
GPV0057 (Compound 5d) is a selective and potent P-glycoprotein (P-gp) inhibitor. GPV0057 is also a selective potassium channel Kir2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of Kir2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, Kir2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome .
loading...
    loading...
Cat. No.: HY-128038
CAS No.: 66164-07-6
Target:  

Opioid Receptor

Research Areas:  

Neurological Disease

N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein .
loading...
    loading...
Cat. No.: HY-155048
CAS No.: 2892824-11-0
Purity:  99.80%
Target:  

Bacterial

Research Areas:  

Infection

BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
loading...
    loading...
Cat. No.: HY-N16577
CAS No.: 928151-78-4
Category:  

Apocynaceae Plants Steroids

Target:  

P-glycoprotein

(S)-Tenacissoside F (Compound P20) is a polyoxypregnane compound found in Marsdenia tenacissima. (S)-Tenacissoside F can inhibit the drug efflux activity mediated by P-glycoprotein (P-gp/ABCB1) and reverse multidrug resistance. (S)-Tenacissoside F can be used for the research of cancer, such as colon cancer .
loading...
    loading...
Cat. No.: HY-P990196

Target:  

P-glycoprotein

Research Areas:  

Cancer

Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
loading...
    loading...
Cat. No.: HY-136940
CAS No.: 2377858-65-4
Target:  

BCRP

Research Areas:  

Cancer

Ac22(Az8)2​ is a selective BCRP inhibitor (EC50: 1-2 nM). Ac22(Az8)2 can restore the drug sensitivity of BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, blocking drug efflux, and increasing intracellular drug accumulation. Ac22(Az8)2 can be used in the research of BCRP-mediated multidrug-resistant cancers .
loading...
    loading...
Cat. No.: HY-D2341
CAS No.: 3055969-34-8
6FC-GABA-Taxol is a fluorescent probe with cell permeability, which is formed by connecting 6FC to the anticancer drug Taxol (HY-B0015) via γ-aminobutyric acid (GABA). 6FC-GABA-Taxol can bind to microtubules in living cells and image them through confocal microscopy. Additionally, 6FC-GABA-Taxol enables the quantification of microtubule binding using flow cytometry without the addition of efflux inhibitors .
loading...
    loading...
Cat. No.: HY-137433A
CAS No.: 2226167-02-6
Synonyms: D-0316 mesylate
Research Areas:  

Inflammation/Immunology Cancer

Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
loading...
    loading...