BAY-876

Catalog No.S8452 Batch:S845201

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Technical Data

Formula

C24H16F4N6O2
Molecular Weight 496.42 CAS No. 1799753-84-6
Solubility (25°C)* In vitro DMSO 99 mg/mL (199.42 mM)
Ethanol 3 mg/mL (6.04 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.
Targets
GLUT1 [1]
(Cell-free assay)
0.002 μM
In vitro

BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1].
In vivo

BAY-876 displays low clearance also in vivo in rat and in dog. The volume of distribution in steady state (Vss) is moderate in both species. Terminal half life is intermediate in rat (2.5 h) and long in dog (22 h) due to the very low clearance. The oral bioavailability (F%) is 85% and 79% in rat and dog, respectively. Preliminary in vivo PK studies of BAY-876 demonstrate that a good oral bioavailability and long terminal half-life is attainable making it an excellent chemical probe to further evaluate the hypothesis of cancer treatment with a very selective GLUT1 inhibitor[1].

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Male Wistar rats

  • Dosages

    0.3 mg/kg

  • Administration

    i.v.

Selleck's BAY-876 has been cited by 18 publications

GLUT1 promotes NLRP3 inflammasome activation of airway epithelium in lipopolysaccharide-induced acute lung injury [ Am J Pathol, 2024, S0002-9440(24)00116-0] PubMed: 38548270
Disulfidptosis-related signature predicts prognosis and characterizes the immune microenvironment in hepatocellular carcinoma [ Cancer Cell Int, 2024, 24(1):19] PubMed: 38195525
Activation of cellular antioxidative stress and migration activities by purified components from immortalized stem cells from human exfoliated deciduous teeth [ Sci Rep, 2024, 14(1):15340] PubMed: 38961142
Alanine supplementation exploits glutamine dependency induced by SMARCA4/2-loss [ Nat Commun, 2023, 14(1):2894] PubMed: 37210563
Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, 4(9):101162] PubMed: 37597521
Metabolic classification suggests the GLUT1/ALDOB/G6PD axis as a therapeutic target in chemotherapy-resistant pancreatic cancer [ Cell Rep Med, 2023, S2666-3791(23)00315-4] PubMed: 37597521
BMP4 upregulates glycogen synthesis through the SMAD/SLC2A1 (GLUT1) signaling axis in hepatocellular carcinoma (HCC) cells [ Cancer Metab, 2023, 11(1):9] PubMed: 37443106
BMP4 upregulates glycogen synthesis through the SMAD/SLC2A1 (GLUT1) signaling axis in hepatocellular carcinoma (HCC) cells [ Cancer Metab, 2023, 11(1):9] PubMed: 37443106
The Impact of Proinflammatory Cytokines and Imiquimod on GLUT1 in HaCaT Keratinocytes - a Potential Anti-Psoriatic Therapeutic Target [ Cell Physiol Biochem, 2023, 57(2):54-62] PubMed: 36945896
Monosodium urate crystals regulate a unique JNK-dependent macrophage metabolic and inflammatory response [ Cell Rep, 2022, 38(10):110489] PubMed: 35263587

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.