A partial agonist of LXRα and LXRβ (Kis = 68 and 14 nM

BMS 779788 – 1 mg

Brand:
Cayman
CAS:
918348-67-1
Storage:
-20
UN-No:
Non-Hazardous - /

BMS 779788 is a partial agonist of liver X receptor α (LXRα) and LXRβ (Kis = 68 and 14 nM, respectively, in a radioligand binding assay).{45493} It activates LXRα and LXRβ with EC50 values of 230 and 250 nM, respectively, in a transactivation assay. BMS 779788 increases expression of ATP-binding cassette transporter (ABCA1) in HeLa cells and isolated human and mouse whole blood (EC50s = 33, 1,200, and 120 nM, respectively). It also increases expression of Abca1 and Abcg2 in isolated mouse blood cells but does not increase plasma or hepatic triglycerides when administered at a dose of 10 mg/kg.  

 

Available on backorder

Add to quotes
SKU: 27339 - 1 mg Category:

Description

A partial agonist of LXRα and LXRβ (Kis = 68 and 14 nM, respectively, in a radioligand binding assay); activates LXRα and LXRβ with EC50 values of 230 and 250 nM, respectively, in a transactivation assay increases expression of ABCA1 in HeLa cells and isolated human and mouse whole blood (EC50s = 33, 1,200, and 120 nM, respectively); increases expression of Abca1 and Abcg2 in mouse blood cells but does not increase plasma or hepatic triglycerides at 10 mg/kg

Formal name: 2-[1-(2-chlorophenyl)-1-methylethyl]-α,α-dimethyl-1-[3′-(methylsulfonyl)[1,1′-biphenyl]-4-yl]-1H-imidazole-4-methanol

Synonyms: 

Molecular weight: 509.1

CAS: 918348-67-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Endocrinology & Metabolism|Hormones & Receptors|FXRs & LXRs

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
    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 – 25 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 - 25 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page
  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 25 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 25 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 – 1 mg

    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 - 1 mg

    Available on backorder

    Add to quotes
    Add to quotes
    View product page