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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
23 Results for "
Caco-2 permeability
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "Caco-2 permeability" in MCE Product Catalog:
2
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
Cat. No.: HY-W040203
CAS No.: 82494-09-5
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Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
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Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
Cat. No.: HY-149408
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MAOA-IN-1 (compound 15) is an orally active MAOA inhibitor with cytotoxicity against prostate cancer cells. MAOA-IN-1 has Caco-2 permeability and lower CNS permeability. MAOA-IN-1 can be further used in the research of anti-cancer and anti-inflammatory indications .
Cat. No.: HY-N6685
CAS No.: 50722-38-8
Synonyms: 3-AcDON; 3-ADON
Cat. No.: HY-178436
Antituberculosis agent-16 is an orally active antituberculosis agent. Antituberculosis agent-16 exhibits stable antituberculosis activity with a MIC of 0.48 μg/mL against Mycobacterium tuberculosis H37Rv sensitive strain and 0.49 μg/mL against multidrug-resistant strain 14862. Antituberculosis agent-16 shows high Caco-2 permeability. Antituberculosis agent-16 can be used for the research of infection .
Cat. No.: HY-156965
CAS No.: 2771756-82-0
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BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
Cat. No.: HY-170491
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GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
Cat. No.: HY-N3197
CAS No.: 477953-07-4
Synonyms: (+)-Neostenine
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Cat. No.: HY-148850
CAS No.: 866598-45-0
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AZD-2207 is a cannabinoid receptor CB1 antagonist, known for its high lipophilicity. AZD-2207 has good intestinal permeability in the Caco-2 model and can be used in research related to type 2 diabetes and obesity .
Cat. No.: HY-P5070
CAS No.: 142155-24-6
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Cat. No.: HY-147397
CAS No.: 1346113-84-5
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PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
(AC50: the concentration which gives 50% activation of enzyme.)
(AC50: the concentration which gives 50% activation of enzyme.)
Cat. No.: HY-131914B
CAS No.: 2088272-67-5
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EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
Cat. No.: HY-128878R
CAS No.: 119817-90-2
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Dexloxiglumide (Standard) is the analytical standard of Dexloxiglumide. This product is intended for research and analytical applications. Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
Cat. No.: HY-159091
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HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
Cat. No.: HY-182459
CAS No.: 198968-25-1
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Org 34167 freebase is a blood-brain barrier permeable HCN channel modulator. Org 34167 freebase possesses high Caco-2 cell permeability. Org 34167 freebase modulates HCN channel function to alter activation properties and suppress neuronal hyperexcitability. Org 34167 freebase induces tremors in mice at specific doses. Org 34167 freebase acts as a research tool for studies on developmental and epileptic encephalopathies as well as depression .
Cat. No.: HY-187358
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Polθ-IN-12 is a DNA polymerase θ (PolQ) polymerase domain inhibitor with a human pIC50 of 8.3. Polθ-IN-12 binds to the allosteric pocket of the PolQ polymerase domain, forming salt bridge interactions with residues Arg-2347 and Arg-2419. Polθ-IN-12 displays improved human metabolic stability and high kinetic solubility at pH 7.4. Polθ-IN-12 shows low CACO-2 permeability and acts as a modest efflux substrate .
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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
