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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
62 Results for "
P-glycoprotein substrate
" in MedChemExpress (MCE) Product Catalog:
Products (62)
62 Results for "P-glycoprotein substrate" in MCE Product Catalog:
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183 Publications Verification
Cat. No.: HY-B0011A
CAS No.: 148408-66-6
Synonyms: RP-56976 Trihydrate
Research Areas:
Docetaxel Trihydrate (RP-56976 Trihydrate) is an orally active tubulin stabilizer with antitumor activity. Docetaxel Trihydrate is a P-glycoprotein substrate and is metabolized by CYP3A to inactive products. Docetaxel Trihydrate binds tubulin, promotes tubulin polymerization, and inhibits microtubule depolymerization. Docetaxel Trihydrate induces aberrant mitosis followed by necrotic-like cell death at low concentrations, and induces G2/M mitotic arrest and drives apoptosis at high concentrations. Docetaxel Trihydrate induces renal injury/renal alterations, sex-dependent granule toxicity/uptake, low cardiac delivery, and decreased hepatic SOD/increased catalase/hepatotoxicity. Docetaxel Trihydrate can be used in cancer-related research .
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Category:
13
Research Areas:
Cardiovascular Disease Infection Neurological Disease Inflammation/Immunology Cancer
Atazanavir (BMS-232632) sulfate is a highly selective and orally active HIV-1 protease inhibitor with blood-brain barrier permeability. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir sulfate inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
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Moxidectin (CL301423) is an orally active and brain-penetrant macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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Category:
Plant Adonis amurensis Regel et Radde Extract Cardiacglycosides Disease Research Fields Inflammation/Immunology Ranunculaceae Extract Steroids
Target:
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1 Cited Publications
Cat. No.: HY-G0017
CAS No.: 404844-02-6
Synonyms: Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588
Research Areas:
N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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Macrolide Antibiotics Antibiotics Cyclopeptides Other Diseases Microorganism Disease Research Antibacterial Disease Research Fields
Target:
Research Areas:
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
Synonyms: CM346
Research Areas:
Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects .
Synonyms: Cordanum
Target:
Research Areas:
Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity .
Cat. No.: HY-142686A
Purity: 96.65%
Target:
Research Areas:
SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis .
Cat. No.: HY-B0011S
CAS No.: 940867-25-4
Synonyms: RP-56976-d9
Research Areas:
Docetaxel-d9 (RP-56976-d9) is the deuterated-labeled Docetaxel (HY-B0011). Docetaxel (RP-56976) is an orally active tubulin stabilizer with antitumor activity. Docetaxel is a P-glycoprotein substrate and is metabolized by CYP3A to inactive products. Docetaxel binds tubulin, promotes tubulin polymerization, and inhibits microtubule depolymerization. Docetaxel induces aberrant mitosis followed by necrotic-like cell death at low concentrations, and induces G2/M mitotic arrest and drives apoptosis at high concentrations. Docetaxel induces renal injury/renal alterations, sex-dependent granule toxicity/uptake, low cardiac delivery, and decreased hepatic SOD/increased catalase/hepatotoxicity. Docetaxel can be used in cancer-related research .
Cat. No.: HY-B0011R
CAS No.: 114977-28-5
Synonyms: RP-56976 (Standard)
Category:
Cat. No.: HY-B0777S
Synonyms: CL-301423-d3
Cat. No.: HY-173162
CAS No.: 86383-89-3
Target:
Research Areas:
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 .
Cat. No.: HY-G0017S
CAS No.: 1185103-28-9
Synonyms: Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8
Cat. No.: HY-128038
CAS No.: 66164-07-6
Target:
Research Areas:
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 .
Cat. No.: HY-142686
CAS No.: 2891696-18-5
Target:
Research Areas:
SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis .
Cat. No.: HY-W001601
CAS No.: 57982-78-2
Target:
Research Areas:
Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
