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Caco‐2

" in MedChemExpress (MCE) Product Catalog:

76

Inhibitors & Agonists

7

Fluorescent Dye

4

Biochemical Assay Reagents

6

Peptides

8

Natural
Products

6

Isotope-Labeled Compounds

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-138068
    L-Tryptophanylglycine

    		Others Metabolic Disease
    L-Tryptophanylglycine (Trp-gly) is a dipeptide that can inhibit Ceronapril uptake by Caco-2 cells, with a Ki of 7.19 mM .
    L-Tryptophanylglycine
  • HY-133948
    1-Monopalmitolein

    Glyceryl palmitoleate

    		 Biochemical Assay Reagents Others
    1-Palmitoleoyl glycerol is a biologically active monoacylglycerol. It increases daunomycin accumulation, shown to inhibit P-glycoprotein in Caco-2 cells. 1-Palmitoleoyl glycerol induces thymocyte apoptosis.
    1-Monopalmitolein
  • HY-14291
    Vildagliptin
    4 Publications Verification

    LAF237; NVP-LAF 237

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease Cancer
    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 .
    Vildagliptin
  • HY-156253
    Anticancer agent 166

    		COX Cancer
    Anticancer agent 166 (compound 3) is an anticancer agent with an excellent inhibition activity against Caco-2 (IC50 = 9.6 nM) .
    Anticancer agent 166
  • HY-121598
    Actisomide

    SC-36602

    		 Apoptosis Cardiovascular Disease
    Actisomide (SC-36602) is an antiarrhythmic agent. Absorption of actisomide in rats and its in vitro uptake in CaCo-2 cells are pH-dependent .
    Actisomide
  • HY-N4236
    Angelol A

    		Others Others
    Angelol A is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model .
    Angelol A
  • HY-13749C
    (S)-Sitagliptin phosphate

    (S)-MK-0431 phosphate

    		 Dipeptidyl Peptidase Autophagy Metabolic Disease
    (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    (S)-Sitagliptin phosphate
  • HY-N4235
    Angelol B

    		Others Inflammation/Immunology
    Angelol B is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model .
    Angelol B
  • HY-13749D
    (Rac)-Sitagliptin

    (Rac)-MK-0431

    		 Autophagy Dipeptidyl Peptidase Metabolic Disease
    (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    (Rac)-Sitagliptin
  • HY-N3197
    Neostenine

    (+)-Neostenine

    		 P-glycoprotein Cancer
    Neostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application [2].
    Neostenine
  • HY-W010162
    H-Ala-Ala-OH

    L-Alanyl-L-alanine; Ala-Ala

    		 Amino Acid Derivatives Others
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) is a nonpolar dipeptide that is absorbed by human intestinal Caco-2 cells. The transport of alanine (Ala), like proton/amino acid symport, can lead to cytoplasmic acidification .
    H-Ala-Ala-OH
  • HY-163042
    HSGN-218

    		Bacterial Infection
    HSGN-218 is an antibacterial agent with low Caco-2 permeability. HSGN-218 efficiently inhibits the growth of different C. difficile species with MIC values ranging from 0.007 μM to 0.07 μM.
    HSGN-218
  • HY-148850
    AZD-2207

    		Cannabinoid Receptor Metabolic Disease
    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 .
    AZD-2207
  • HY-14291A
    Vildagliptin dihydrate

    LAF237 dihydrate; NVP-LAF 237 dihydrate

    		 Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease Cancer
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity .
    Vildagliptin dihydrate
  • HY-13749CR
    (S)-Sitagliptin phosphate (Standard)

    (S)-MK-0431 phosphate (Standard)

    		 Reference Standards Dipeptidyl Peptidase Autophagy Metabolic Disease
    (S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    (S)-Sitagliptin phosphate (Standard)
  • HY-P4296
    H-Gly-Sar-Sar-OH

    		Amino Acid Derivatives Others
    H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation [2] .
    H-Gly-Sar-Sar-OH
  • HY-14291S1
    Vildagliptin-d7

    LAF237-d7; NVP-LAF 237-d7

    		 Isotope-Labeled Compounds Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d7 is deuterium labeled Vildagliptin. 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 .
    Vildagliptin-d7
  • HY-14291S
    Vildagliptin-d3

    LAF237-d3; NVP-LAF 237-d3

    		 Isotope-Labeled Compounds Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d3 is the deuterium labeled Vildagliptin. 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 [2].
    Vildagliptin-d3
  • HY-20808
    Antioxidant agent-15

    		COX Cancer
    Antioxidant agent-15 (Compound 4) is a potent antioxidant inhibition activity, with the IC50 of 15.44 nM. Antioxidant agent-15 inhibits tumor cell growth in Hela, Hep G2 and Caco-2 cells, with the IC50 of 395.26, 400.4 and 24.6 nM, respectively .
    Antioxidant agent-15
  • HY-149408
    MAOA-IN-1

    		Monoamine Oxidase Cancer
    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 .
    MAOA-IN-1
  • HY-14291R
    Vildagliptin (Standard)

    LAF237 (Standard); NVP-LAF 237 (Standard)

    		 Reference Standards Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (Standard) is the analytical standard of Vildagliptin. This product is intended for research and analytical applications. 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 .
    Vildagliptin (Standard)
  • HY-D0300
    Leucomalachite green
    1 Publications Verification

    		 Biochemical Assay Reagents Others
    Leucomalachite green is the major reduced metabolite of malachite green (MG) and has lower cytotoxicity (such as HEp-2 and Caco-2) than malachite green. Leucomalachite green may be involved in interfering with cell metabolism or redox balance and can be used to evaluate its potential harm to human cells as a food contaminant [2].
    Leucomalachite green
  • HY-14291B
    (2R)-Vildagliptin

    (2R)-LAF237; (2R)-NVP-LAF 237

    		 Dipeptidyl Peptidase Metabolic Disease
    (2R)-Vildagliptin is the isomer of Vildagliptin (HY-14291), and can be used as an experimental control. 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 .
    (2R)-Vildagliptin
  • HY-W011053
    Neotame

    		Taste Receptor Apoptosis Drug Derivative Metabolic Disease
    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] .
    Neotame
  • HY-14291S5
    Vildagliptin-d6

    LAF237-d6 ; NVP-LAF 237-d6

    		 Isotope-Labeled Compounds Apoptosis Ferroptosis Dipeptidyl Peptidase Metabolic Disease Cancer
    Vildagliptin-d6 (LAF237-d6 ) is deuterium labeled Vildagliptin. 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 .
    Vildagliptin-d6
  • HY-156526
    PHD-IN-1

    		HIF/HIF Prolyl-Hydroxylase Others
    PHD-IN-1 (compound 80) is a potent inhibitor of PHD2，with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells，respectively .
    PHD-IN-1
  • HY-161845
    Anticancer agent 240

    		Drug Derivative Cancer
    Anticancer agent 240 (compound 9b) is an 8-quinolinesulfonamide derivative with a cytotoxicity activity. Anticancer agent 240 shows inhibitory activity in Caco-2, SNB-19, A-549, and SKOV-3 cell line IC50 values of 0.26, 0.38, 0.40 and 4.16 μM .
    Anticancer agent 240
  • HY-P5038
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)

    c(GRGDSP)

    		 Integrin Cancer
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)
  • HY-116788
    Lipofermata
    Maximum Cited Publications
    8 Publications Verification

    		 Bacterial Infection
    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] .
    Lipofermata
  • HY-147397
    PKM2 activator 3

    		Pyruvate Kinase Cancer
    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.)
    PKM2 activator 3
  • HY-N2009
    3-O-Methylgallic acid

    3,4-Dihydroxy-5-methoxybenzoic acid

    		 Apoptosis Caspase Cancer
    3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects [2] .
    3-O-Methylgallic acid
  • HY-131914B
    EST64454 maleate

    		Sigma Receptor Inflammation/Immunology
    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.
    EST64454 maleate
  • HY-173367
    Anticancer agent 271

    		EGFR PI3K mTOR Cancer
    Anticancer agent 271 (compound 5C) has antiproliferative activity against lung (A549), colon (Caco-2) cancer cell lines, and human lung fibroblast (WI38) with an IC50 value of 9.18 μM on A549 cells. Anticancer agent 271 downregulates PI3K and mTOR gene expression that can be used for cancer research .
    Anticancer agent 271
  • HY-146078
    Antimicrobial agent-1

    		Bacterial Infection
    Antimicrobial agent-1 (compound 6C) possesses potent activity against TolC mutant E. coli with an MIC value of 2 μg/mL. Antimicrobial agent-1 and Colistin exhibit synergistic activity against Gram-negative bacteria. Antimicrobial agent-1 has no cytotoxicity on mammalian cell lines, with MICs > 128 μg/mL in Caco-2 and Vero cell lines .
    Antimicrobial agent-1
  • HY-162239
    Anticancer agent 187

    		Others Cancer
    Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
    Anticancer agent 187
  • HY-111956
    D-Ala-Lys-AMCA

    		Fluorescent Dye Cancer
    D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) [2].
    D-Ala-Lys-AMCA
  • HY-D0300S1
    Leucomalachite green-d6

    		Isotope-Labeled Compounds Biochemical Assay Reagents Others
    Leucomalachite green-d6 is the deuterated derivative of Leucomalachite green (HY-D0300). Leucomalachite green is the major reduced metabolite of malachite green (MG) and has lower cytotoxicity (such as HEp-2 and Caco-2) than malachite green. Leucomalachite green may be involved in interfering with cell metabolism or redox balance and can be used to evaluate its potential harm to human cells as a food contaminant [2].
    Leucomalachite green-d6
  • HY-111956B
    D-Ala-Lys-AMCA hydrochloride
    1 Publications Verification

    		 Fluorescent Dye Cancer
    D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) [2].
    D-Ala-Lys-AMCA hydrochloride
  • HY-D0300S
    Leucomalachite green-d5

    		Isotope-Labeled Compounds Biochemical Assay Reagents Others
    Leucomalachite green-d5 is the deuterated derivative of Leucomalachite green (HY-D0300). Leucomalachite green is the major reduced metabolite of malachite green (MG) and has lower cytotoxicity (such as HEp-2 and Caco-2) than malachite green. Leucomalachite green may be involved in interfering with cell metabolism or redox balance and can be used to evaluate its potential harm to human cells as a food contaminant [2].
    Leucomalachite green-d5
  • HY-172112
    VEGFR-2-IN-64

    		VEGFR Apoptosis Cancer
    VEGFR-2-IN-64 (Compound 28) is the inhibitor for VEGFR2 with IC50 of 27.8 nM. VEGFR-2-IN-64 inhibits the proliferation of cancer cell A549, T-47D and Caco-2, exhibits anti-migration and anti-cloning activities in cell T-47D, induces apoptosis in T-47D .
    VEGFR-2-IN-64
  • HY-169477
    PAMAM dendrimer G0.5 carboxylate sodium

    		Biochemical Assay Reagents Cancer
    PAMAM Dendrimer G0.5 Carboxylate sodium is a polyamidoamine (PAMAM) dendrimer with carboxylate termini. PAMAM Dendrimer G0.5 Carboxylate sodium conjugated with DACHPt is cytotoxic to A2780 ovarian cancer cells, MCF-7 breast cancer cells, Caco-2 colon cancer cells and BJ fibroblasts with IC50 values of 0.03, 1.6, 0.18 and 3 µM, respectively .
    PAMAM dendrimer G0.5 carboxylate sodium
  • HY-111956A
    D-Ala-Lys-AMCA TFA

    		Fluorescent Dye Cancer
    D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors (Ex/Em = 390/480 nm) [2].
    D-Ala-Lys-AMCA TFA
  • HY-178436
    Antituberculosis agent-16

    		Bacterial Infection
    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 .
    Antituberculosis agent-16
  • HY-128878
    Dexloxiglumide

    		Cholecystokinin Receptor P-glycoprotein Metabolic Disease Endocrinology
    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] .
    Dexloxiglumide
  • HY-155337
    eIF4E-IN-6

    		Eukaryotic Initiation Factor (eIF) Cancer
    eIF4E-IN-6(compound 4b) is a GMP analogs synthesized to targeteIF4Eand restrain its binding to cap mRNA.eIF4E-IN-6shows cell cytotoxicity against Caco-2, HepG-2,and MCF-7 cells, withIC50values of 31, 27, and 21 μM, respectively .
    eIF4E-IN-6
  • HY-156965
    BAY-771

    		Fluorescent Dye Metabolic Disease Cancer
    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 .
    BAY-771
  • HY-W011053GL
    Neotame (GMP Like)

    		Taste Receptor Apoptosis Drug Derivative Metabolic Disease
    Neotame (GMP Like) is the GMP Like class Neotame (HY-W011053) that can be used as pharmaceutical excipients. 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] .
    Neotame (GMP Like)
  • HY-P10329
    KK14(R)

    		Fungal Infection
    KK14(R) is an analog of the de novo synthetic peptide KK14, which exhibits antifungal activity against Fusarium culmorum, Penicillium expansum and Aspergillus niger , with MICs of 6.25, 12.5 and 12.5 μg/mL, respecitvely. KK14(R) exhibits good heat- and pH-stability. KK14(R) exhibits cytotoxicity against cells Caco-2 and RAW264.7 .
    KK14(R)
  • HY-W011053R
    Neotame (Standard)

    		Apoptosis Drug Derivative Reference Standards Metabolic Disease
    Neotame (Standard) is the analytical standard of Neotame (HY-W011053). This product is intended for research and analytical applications. 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] .
    Neotame (Standard)
  • HY-D0300R
    Leucomalachite green (Standard)

    		Biochemical Assay Reagents Reference Standards Others
    Leucomalachite green (Standard) is the analytical standard of Leucomalachite green (HY-D0300). This product is intended for research and analytical applications. Leucomalachite green is the major reduced metabolite of malachite green (MG) and has lower cytotoxicity (such as HEp-2 and Caco-2) than malachite green. Leucomalachite green may be involved in interfering with cell metabolism or redox balance and can be used to evaluate its potential harm to human cells as a food contaminant [2].
    Leucomalachite green (Standard)

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