Phenelzine-d5 (sulfate) is intended for use as an internal standard for the quantification of phenelzine (Item No. 23956) by GC- or LC-MS. Phenelzine is an inhibitor of monoamine oxidase (MAO; IC50 = 0.9 μM using rat brain mitochondrial preparations).{38498} It potentiates the effects of tryptamine on isolated rat fundus (EC50 = 90 nM) and increases tryptamine toxicity in mice with LD50 values of 85 and 500 mg/kg in the presence and absence of phenelzine, respectively. Phenelzine (20 mg/kg) increases GABA, dopamine, serotonin (5-HT; Item No. 14332), and norepinephrine levels in the hippocampus and cortex of socially isolated rats and rats treated with the NMDA receptor antagonist (+)-MK-801 (Item No. 10009019).{38499} It also increases 5-HT levels in the ventral horn of the spinal cord, improves gross motor ability in a rotarod test, and increases locomotor activity in an open field test in mice with experimental autoimmune encephalomyelitis when administered at a dose of 30 mg/kg.{38500}
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An internal standard for the quantification of phenelzine by GC- or LC-MS,,
Formal name: (2-phenylethyl-d5)-hydrazine, monosulfate
Synonyms:
Molecular weight: 239.3
CAS: 1219798-40-9
Purity: ≥99% deuterated forms (d1-d5)
Formulation: A solid
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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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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