Ziprasidone-d8 is intended for use as an internal standard for the quantification of ziprasidone (Item No. 15031) by GC- or LC-MS. Ziprasidone is an atypical antipsychotic.{26444} It is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 36.31 nM for inhibition of forskolin-induced adenylate cyclase activity in HeLa cells expressing human receptors), as well as an inverse agonist of 5-HT1D receptors (IC50 = 2.69 nM) and a partial agonist of 5-HT1B receptors (EC50 = 6.17 nM) in [35S]GTPγS binding assays.{54360,22640} Ziprasidone is an antagonist at 5-HT2A and dopamine D2 receptors (Kis = 1.15 and 1.29 nM, respectively) in cell-based assays.{54361} It inhibits d-amphetamine-induced hyperactivity and apomorphine-induced stereotypy in rats (ID50s = 1.53 and 2.43 mg/kg, respectively). Formulations containing ziprasidone have been used in the treatment of schizophrenia and bipolar I disorder.
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An internal standard for the quantification of ziprasidone by GC- or LC-MS
Formal name: 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl-2,2,3,3,5,5,6,6-d8]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one
Synonyms: CP-88,059-d8
Molecular weight: 421
CAS: 1126745-58-1
Purity: ≥99% deuterated forms (d1-d8)
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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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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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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