Buproprion (Item No. 10488) is an inhibitor of the reuptake of dopamine and norepinephrine and is also an antagonist of neuronal acetylcholine nicotinic receptors. Because of its effects on nicotinic receptors, it is used to promote smoking cessation. Hydroxy bupropion is a mixture of enantiomers produced by the metabolism of buproprion by cytochrome P450 2B6.{22910,22909} Compared with buproprion, this racemic mixture produces equal inhibition of norepinephrine reuptake (IC50 = 1.7 µM) and much weaker inhibition of dopamine reuptake (IC50 >10 µM).{22912} Moreover, hydroxyl bupropion isomers are potent antagonists of nicotinic receptors, suggesting that they may substitute for bupropion in smoking cessation.{22912,22911,22909}
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A mixture of enantiomers produced by the metabolism of buproprion by cytochrome P450 2B6; potently inhibits norepinephrine reuptake (IC50 = 1.7 µM) with much weaker inhibition of dopamine reuptake (IC50 >10 µM); potently antagonizes nicotinic receptors
Formal name: 2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol
Synonyms:
Molecular weight: 255.7
CAS: 357399-43-0
Purity: ≥98%
Formulation: A crystalline 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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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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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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