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Results for "

KGA

" in MedChemExpress (MCE) Product Catalog:

7

Inhibitors & Agonists

1

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-123797
    KGA-2727
    1 Publications Verification

    SGLT Metabolic Disease
    KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy .
    KGA-2727
  • HY-17638
    Mizagliflozin
    3 Publications Verification

    DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base

    SGLT Metabolic Disease
    Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation .
    Mizagliflozin
  • HY-114334
    Glutaminase-IN-1
    1 Publications Verification

    CB839 derivative

    Glutaminase Cancer
    Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
    Glutaminase-IN-1
  • HY-12248
    Telaglenastat
    Maximum Cited Publications
    70 Publications Verification

    CB-839

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
    Telaglenastat
  • HY-17638A

    DSP-3235 (sebacate); KGA-3235 (sebacate); GSK-1614235 (sebacate)

    SGLT Neurological Disease
    Mizagliflozin sebacate (DSP-3235 sebacate) is a sodium-glucose cotransporter inhibitor with activity in improving vascular cognitive impairment caused by small vessel disease. Mizagliflozin sebacate improves blood flow and reverses vascular cognitive impairment by inhibiting neuronal SGLT1 activity. Mizagliflozin sebacate also showed the ability to increase the survival rate of IL-1β-treated PC12HS cells. Mizagliflozin sebacate promotes improvements in spatial learning and memory caused by small vessel disease in mouse models .
    Mizagliflozin (sebacate)
  • HY-158378

    R-AST-OH

    Glutaminase Cancer
    Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
    Trivalent hydroxyarsinothricn
  • HY-12248A

    CB-839 hydrochloride

    Glutaminase Autophagy Cancer
    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
    Telaglenastat hydrochloride

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