Nateglinide-d5 is intended for use as an internal standard for the quantification of nateglinide (Item No. 23320) by GC- or LC-MS. Nateglinide is a hypoglycemic agent.{38370,38371,38372} It induces insulin and somatostatin release from perfused rat pancreas when used at concentrations ranging from 0.03 to 3 μM.{38370} Nateglinide (3 µM) increases intracellular calcium levels in isolated rat pancreatic β cells, an effect that can be inhibited by the L-type calcium channel blocker nitrendipine (Item No. 17549). Nateglinide-induced secretion of insulin and somatostatin and calcium influx is also reversed by the potassium channel activator diazoxide (Item No. 14576). Oral administration of nateglinide (1.6 mg/kg) reduces blood glucose levels by 20% in fasted mice.{38371} It also decreases blood glucose levels in an oral glucose tolerance test in normal rats, genetically diabetic KK mice, and a rat model of diabetes induced by streptozotocin (STZ; Item No. 13104).{38372} Formulations containing nateglinide have been used in the treatment of type 2 diabetes.
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An internal standard for the quantification of nateglinide by GC- or LC-MS
Formal name: N-[[trans-4-(1-methylethyl)cyclohexyl]carbonyl]-D-phenylalanine-2,3,4,5,6-d5
Synonyms:
Molecular weight: 322.5
CAS: 1227666-13-8
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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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 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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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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