Paliperidone-d4 is intended for use as an internal standard for the quantification of paliperidone (Item No. 15556) by GC- or LC-MS. Paliperidone is an atypical antipsychotic.{42913} It is an inverse agonist of dopamine D2 and D3 receptors (IC50s = 1 and 0.9 nM, respectively), as well as an antagonist at these receptors (Kis = 0.4 and 0.1 nM, respectively).{25512} Paliperidone also binds to α1- and α2-adrenergic receptors, histamine H1 receptors, and the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C (Kds = 10.1, 80, 3.4, 480, 19, 1.21, and 48 nM, respectively).{25511} It improves spatial working memory in a T-maze alternation task in a maternal immune activation mouse model of schizophrenia when administered at a dose of 0.05 mg/kg per day.{42913} Paliperidone is also an active metabolite of the atypical antipsychotic risperidone (Item No. 13629).{25511} Formulations containing paliperidone have been used in the treatment of schizophrenia and schizoaffective disorder.
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An internal standard for the quantification of paliperidone by GC- or LC-MS
Formal name: 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl-1,1,2,2-d4]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
Synonyms: 9-hydroxy Risperidone-d4
Molecular weight: 430.5
CAS: 1020719-55-4
Purity: ≥99% deuterated forms (d1-d4)
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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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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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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