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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
106 Results for "
Caco2
" in MedChemExpress (MCE) Product Catalog:
Products (106)
106 Results for "Caco2" in MCE Product Catalog:
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9 Publications Verification
Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM [2] .
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5 Cited Publications
Synonyms: LAF237; NVP-LAF 237
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Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
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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 [2].
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1 Cited Publications
Cat. No.: HY-W127512
CAS No.: 546-18-9
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5β-Cholanic acid is a hydrophobic modifier used to modify polymer carriers. 5β-Cholanic acid can improve the acid stability, cell penetration efficiency and drug sustained release ability of nanocarriers, and optimize the oral effectiveness of delivered molecules. 5β-Cholanic acid can covalently bind to Glycol chitosan (GC) to form a GC-CA conjugate, which optimizes the hydrophobic anchoring ability of nanoparticles and enables them to be stably adsorbed on the surface of PLGA nanoparticles. Such nanoparticles can resist dissociation in the gastric acid environment and maintain positive charge to enhance endocytic uptake by intestinal epithelial cells (such as Caco-2 cells). 5β-Cholanic acid can be used in the development of drug delivery systems [2].
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Promethazine is an orally active histamine receptor antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects [2] .
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1 Cited Publications
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1 Cited Publications
Synonyms: Glyceryl palmitoleate
Cat. No.: HY-W011053
CAS No.: 165450-17-9
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Neotame is a derivative of Aspartame (HY-B0361) and is a flavor enhancer and low-caloric, non-nutritive, high-intensity artificial sweetener that is 7000-13,000 times sweeter than sugar. Neotame causes intestinal epithelial cell death at high concentrations. Neotame induces Apoptosis of Caco-2 cells [2] .
Cat. No.: HY-W009141
CAS No.: 542-44-9
Synonyms: Glyceryl palmitate
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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 [2] .
Cat. No.: HY-170522
CAS No.: 2924181-80-4
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ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases .
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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-W014701
CAS No.: 31519-22-9
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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-111956
CAS No.: 375822-19-8
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Cat. No.: HY-155328
CAS No.: 3032392-39-2
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GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice .
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
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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
