A prodrug form of telotristat; reduces levels of 5-HT in mouse jejunum and blood at 15-300 mg/kg; inhibits increases in IL-1β and IL-6 levels

Telotristat Etiprate – 25 mg

Brand:
Cayman
CAS:
1137608-69-5
Storage:
-20
UN-No:
Non-Hazardous - /

Telotristat etiprate is a prodrug form of telotristat, which is an inhibitor of tryptophan hydroxylase 1 (TPH1).{43269} Telotristat etiprate (15-300 mg/kg) reduces levels of serotonin (5-HT; Item No. 14332) in mouse jejunum and blood but not brain.{43270} It inhibits increases in IL-1β and IL-6 levels, histological damage in the colon, and weight loss in a mouse model of trinitrobenzene sulfonic acid-induced colitis when administered at a dose of 200 mg/kg. In mice infected with the nematode T. muris, telotristat etiprate (300 mg/kg per day) reduces colonic levels of myeloperoxidase (MPO), IL-1β, and IL-17, as well as worm burden.{43271} Formulations containing telotristat etiprate have been used in the treatment of diarrhea associated with carcinoid syndrome.  

 

Available on backorder

Add to quotes
SKU: 25342 - 25 mg Category:

Description

A prodrug form of telotristat; reduces levels of 5-HT in mouse jejunum and blood at 15-300 mg/kg; inhibits increases in IL-1β and IL-6 levels, histological damage in the colon, and weight loss in a mouse model of trinitrobenzene sulfonic acid-induced colitis at 200 mg/kg; reduces colonic levels of MPO, IL-1β, and IL-17, as well as worm burden, in mice infected with T. muris at 300 mg/kg

Formal name: 4-[2-amino-6-[(1R)-1-[4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl]-2,2,2-trifluoroethoxy]-4-pyrimidinyl]-L-phenylalanine, ethyl ester, compd. with N-benzoylglycine

Synonyms:  LX 1032 hippurate|LX 1606 hippurate

Molecular weight: 754.2

CAS: 1137608-69-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Immunology & Inflammation|Gastric Disease||Research Area|Infectious Disease|Parasitic Diseases

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 – 10 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 - 10 mg

    Available on backorder

    Add to quotes
    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
    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 5 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 5 mg

    Available on backorder

    Add to quotes
    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
    Add to quotes
    View product page