Atomoxetine-d3 is intended for use as an internal standard for the quantification of atomoxetine (Item No. 22248) by GC- or LC-MS. Atomoxetine is a selective norepinephrine reuptake inhibitor with Ki values of 5, 77, and 1,451 nM for norepinephrine, serotonin, and dopamine transporters, respectively.{38422} It is selective over the choline, GABA, and adenosine transporters, and a number of neurotransmitter receptors, ion channels, second messengers, and brain/gut peptides. In the rat prefrontal cortex (PFC), it increases extracellular norepinephrine and dopamine by 3-fold and increases Fos expression. Atomoxetine (0.1, 0.5, and 1 mg/kg) reduces premature responding, a measure of impulsivity, by rats in the 5-choice serial reaction time test (5CRTT) in a dose-dependent manner.{38421} It also has neuroprotective effects when administered prior to ischemic damage in a gerbil model of transient cerebral ischemia.{38423} Formulations containing atomoxetine have been used in the treatment of attention-deficit hyperactivity disorder (ADHD) in children, adolescents, and adults.
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An internal standard for the quantification of atomoxetine by GC- or LC-MS
Formal name: (R)-N-(methyl-d3)-3-phenyl-3-(o-tolyloxy)propan-1-amine, monohydrochloride
Synonyms:
Molecular weight: 294.8
CAS: 1217776-38-9
Purity: ≥99% deuterated forms (d1-d3)
Formulation: A solid
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.
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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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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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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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