An aldose reductase inhibitor (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase

Epalrestat – 5 mg

Brand:
Cayman
CAS:
82159-09-9
Storage:
-20
UN-No:
Non-Hazardous - /

Epalrestat is an inhibitor of aldose reductase (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively).{53254} It inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC50s = 1.5, 5, and 1.5 µM, respectively). It decreases high glucose-induced proliferation of vascular smooth muscle cells when used at a concentration of 10 nM and prevents high glucose-induced intracellular NADH/NAD+ increases and membrane-bound PKC activation at 100 nM.{24663,24664} Epalrestat (20 and 40 mg/kg) improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy.{53255} It also prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy when administered at a dose of 50 mg/kg.{53256}  

 

Add to quotes
SKU: - Category:

Description

An aldose reductase inhibitor (IC50s = 0.01 and 0.26 µM for rat lens and human placenta aldose reductase, respectively); inhibits glucose-induced sorbitol accumulation in isolated rat lens, rat sciatic nerve, and human erythrocytes (IC50s = 1.5, 5, and 1.5 µM, respectively); decreases high glucose-induced proliferation of vascular smooth muscle cells at 10 nM and prevents high glucose-induced intracellular NADH/NAD+ increases and membrane-bound PKC activation at 100 nM; improves motor nerve conduction velocity and decreases sorbitol content in the sciatic nerve and erythrocytes in a rat model of streptozotocin-induced diabetic neuropathy at 20 and 40 mg/kg; prevents capillary strand formation in a rat model of diabetes-induced retinal microangiopathy at 50 mg/kg

Formal name: 5Z-[(2E)-2-methyl-3-phenyl-2-propen-1-ylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid

Synonyms:  ONO-2235

Molecular weight: 319.4

CAS: 82159-09-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cardiovascular System|Vasculature|Smooth Muscle Cells||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Neuroscience

Related products

  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 50 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 100 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 25 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 25 µg

    Available on backorder

    Add to quotes
    View product page
  • A powerful effector in both the TetR and revTetR transcriptional regulator systems

    Anhydrotetracycline (hydrochloride) – 50 mg

    The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}  

     

    Brand:
    Cayman
    SKU:10009542 - 50 mg

    Available on backorder

    Add to quotes
    View product page