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Results for "

gut-restricted

" in MedChemExpress (MCE) Product Catalog:

13

Inhibitors & Agonists

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135747
    Gut restricted-7
    Maximum Cited Publications
    6 Publications Verification

    GR-7

    		 Bacterial Infection
    Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice .
    Gut restricted-7
  • HY-126855
    Cholic acid 7-sulfate
    1 Publications Verification

    7-Sulfocholic acid

    		 G protein-coupled Bile Acid Receptor 1 MHC Metabolic Disease
    Cholic acid 7-sulfate (7-Sulfocholic acid) is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
    Cholic acid 7-sulfate
  • HY-12820
    Sibofimloc
    4 Publications Verification

    Antibiotic-202

    		 Bacterial Antibiotic Infection
    Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD) .
    Sibofimloc
  • HY-141521
    Amelenodor
    2 Publications Verification

    NX-13

    		 NOD-like Receptor (NLR) Inflammation/Immunology
    NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis .
    Amelenodor
  • HY-109148
    Izencitinib

    TD-1473; JNJ-8398

    		 JAK Inflammation/Immunology
    Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor. Izencitinib (TD-1473) can be used in the study for ulcerative colitis .
    Izencitinib
  • HY-156685
    EDI048

    		PI4K Parasite Infection Metabolic Disease Cancer
    EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
    EDI048
  • HY-178028
    PRMT5-IN-53

    		Histone Methyltransferase Cancer
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
    PRMT5-IN-53
  • HY-168329
    TGR5 agonist 7

    		G protein-coupled Bile Acid Receptor 1 Metabolic Disease
    TGR5 agonist 7 (Compound 22-Na) is a gut-restricted, orally active agonist for G protein-coupled bile acid receptor TGR5 (GPBAR1 or GPR131) with an EC50 < 1 μM. TGR5 agonist 7 exhibits blood glucose lowering effect in mouse model, and can be used in diabete research .
    TGR5 agonist 7
  • HY-12820R
    Sibofimloc (Standard)

    Antibiotic-202 (Standard)

    		 Reference Standards Bacterial Antibiotic Infection
    Sibofimloc (Standard) is the analytical standard of Sibofimloc. This product is intended for research and analytical applications. Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD)[1][2].
    Sibofimloc (Standard)
  • HY-115866
    COX-2-IN-6

    		COX Cancer
    COX-2-IN-6 (compound 10) is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. COX-2-IN-6 selectively targets COX-2 with an IC50 of 0.84 μM and a Ki of 69 nM. COX-2-IN-6 also inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM .
    COX-2-IN-6
  • HY-126855S
    Cholic acid 7-sulfate-d4

    7-Sulfocholic acid-d4

    		 Isotope-Labeled Compounds G protein-coupled Bile Acid Receptor 1 MHC Metabolic Disease
    Cholic acid 7-sulfate-d4 (7-Sulfocholic acid-d4) is the deuterium labeled Cholic acid 7-sulfate (HY-126855). Cholic acid 7-sulfate is a selective agonist targeting TGR5 (EC50=0.17 μM) and a ligand for MHC class I-related protein (MR1). As a gut-restricted TGR5 agonist, cholic acid 7-sulfate binds to TGR5 on enteroendocrine L cells, induces GLP-1 secretion, and improves glucose tolerance in a TGR5-dependent manner. Cholic acid 7-sulfate also acts as an endogenous ligand for MR1, promoting the survival of mucosal-associated invariant T cells MAIT and the expression of homeostatic gene signatures, affecting MAIT cell development and function. Cholic acid 7-sulfate is mainly used in the research of diabetes and MAIT cell-related immune regulation .
    Cholic acid 7-sulfate-d4
  • HY-181872
    JAK1-IN-20

    		JAK Interleukin Related STAT Inflammation/Immunology
    JAK1-IN-20 (Compound 38) is a gut-restricted, orally active, selective JAK1 inhibitor with an IC50 of <0.5 nM. JAK1-IN-20 inhibits the enzymatic activity of JAK1, reduces the production of proinflammatory cytokines (TNF-α, IL-6), and suppresses the phosphorylation of STAT3. JAK1-IN-20 ameliorates ulcerative colitis. JAK1-IN-20 can be used for the research of inflammatory bowel disease .
    JAK1-IN-20
  • HY-181876
    F44-S101

    		FXR Metabolic Disease
    F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia .
    F44-S101

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