Many of the effects of prostaglandin D2 (PGD2) are transduced via a traditional 7-transmembrane GPCR, the DP1 receptor.{3128} However, in certain leukocytes and other immune cells, a second PGD2 receptor referred to as the CRTH2 or DP2 receptor has been cloned and characterized.{9767,9769} 15(R)-15-methyl PGD2 is a surprisingly potent agonist at the DP2 receptor, being about 5 times more potent than PGD2 itself.{10723} 15(R)-PGD2 has the potential to be produced endogenously as a natural ligand for DP2, unlike the synthetic 15-methyl analogs. In preliminary reports, 15(R)-PGD2 has also been reported to be a potent and selective DP2 receptor agonist.{11220,14546}
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A potent and selective CRTH2/DP2 receptor agonist, that is equipotent with PGD2 at this receptor
Formal name: 9α,15R-dihydroxy-11-oxo-prosta-5Z,13E-dien-1-oic acid
Synonyms: 15(R)-PGD2
Molecular weight: 352.5
CAS: 59894-05-2
Purity: ≥98%
Formulation: A solution in methyl acetate
Product Type|Biochemicals|Lipids|Prostaglandins||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway
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}
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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}
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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}
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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}
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