An agonist of GPR40/FFA1 (EC50 = 47.8 nM); selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3

GW 9508 – 50 mg

Brand:
Cayman
CAS:
885101-89-3
Storage:
-20
UN-No:
Non-Hazardous - /

GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}  

 

Available on backorder

Add to quotes
SKU: 10008907 - 50 mg Category:

Description

An agonist of GPR40/FFA1 (EC50 = 47.8 nM); selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM); potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 cells; activates AMPK-ACC signaling; decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis at 100 mg/kg per day for three days

Formal name: 4-[[(3-phenoxyphenyl)methyl]amino]-benzenepropanoic acid

Synonyms: 

Molecular weight: 347.4

CAS: 885101-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Lipid Biochemistry|Acyl-CoAs||Research Area|Lipid Biochemistry|Fatty Acids

Related products

  • 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 – 1 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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 500 µg

    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
  • 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
    Add to quotes
    View product page