A potent agonist of GPR35 (EC50 = 1.61 nM); inhibits histamine release in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM); inhibits A23187-induced calcium influx in isolated rat mast cells; reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml; dose-dependently reduces the immediate hypersensitivity response in rat conjunctiva in vivo; reduces mast cell degranulation in rat conjunctiva

Lodoxamide – 250 mg

Brand:
Cayman
CAS:
53882-12-5
Storage:
-20
UN-No:
Non-Hazardous - /

Lodoxamide is a potent agonist of GPR35 with an EC50 value of 1.61 nM in a β-arrestin-2 interaction assay using CHO-K1 cells expressing the human receptor.{38490} It inhibits histamine release induced by compound 48/80 (Item No. 22173), anti-IgE, or A23187 (Item No. 11016) in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM) and inhibits A23187-induced calcium influx in mast cells.{38491} It reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml.{38492} Lodoxamine (0.1 and 10%, w/v) reduces the immediate hypersensitivity response in rat conjunctiva in vivo in a dose-dependent manner and reduces mast cell degranulation in a topical ovalbumin challenge.{38492,38493} Formulations containing lodoxamide have been used in the treatment of vernal conjunctivitis and keratitis.  

 

Available on backorder

Add to quotes
SKU: 23994 - 250 mg Category:

Description

A potent agonist of GPR35 (EC50 = 1.61 nM); inhibits histamine release in isolated rat peritoneal mast cells (IC50s = 0.1-50 µM); inhibits A23187-induced calcium influx in isolated rat mast cells; reduces antigen-induced histamine release from rat conjunctival tissue by 46% in vitro when used at a concentration of 10 µg/ml; dose-dependently reduces the immediate hypersensitivity response in rat conjunctiva in vivo; reduces mast cell degranulation in rat conjunctiva

Formal name: 2,2′-[(2-chloro-5-cyano-1,3-phenylene)diimino]bis[2-oxo-acetic acid]

Synonyms: 

Molecular weight: 311.6

CAS: 53882-12-5

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 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 - 50 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 – 5 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 - 5 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 – 10 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 - 10 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 – 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