Aripiprazole-d8 is intended for use as an internal standard for the quantification of aripiprazole (Item No. 19989) by GC- or LC-MS. Aripiprazole is an atypical antipsychotic.{47557} It is a partial agonist at dopamine D2, D2L, and D3 receptors (Kis = 3.3, 0.74, 9.7 nM, respectively), a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 5.6 nM), and an inverse agonist of 5-HT2B receptors (Ki = 0.36 nM). It is functionally selective at the dopamine D2 receptor with cell-type- and function-selective activities. Aripiprazole inhibits disruptions in prepulse inhibition induced by phencyclidine in mice when administered at doses of 5 and 10 mg/kg.{47558} Formulations containing aripiprazole have been used in the treatment of schizophrenia, bipolar mania or mixed episodes, and Tourette’s disorder.
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An internal standard for the quantification of aripiprazole by GC- or LC-MS
Formal name: 7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy-1,1,2,2,3,3,4,4-d8]-3,4-dihydro-2(1H)-quinolinone
Synonyms:
Molecular weight: 456.4
CAS: 1089115-04-7
Purity: ≥99% deuterated forms (d1-d8)
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 tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
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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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