Fosinopril-d7 is intended for use as an internal standard for the quantification of fosinopril (Item No. 21899) by GC- or LC-MS. Fosinopril is a prodrug form of the angiotensin-converting enzyme (ACE) inhibitor fosinoprilat.{39303} Oral administration of fosinopril inhibits angiotensin I-induced pressor responses in normotensive rats, dogs, and monkeys when administered at doses of 15, 15, and 10 µmol/kg, respectively. Fosinopril (2.5 mg/kg) reduces fractional shortening and decreases left ventricular size in a porcine model of congestive heart failure.{39770} Formulations containing fosinopril have been used in the treatment of hypertension and congestive heart failure.
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An internal standard for the quantification of fosinopril by GC- or LC-MS
Formal name: (2S,4S)-4-cyclohexyl-1-(2-((R)-((S)-2-methyl-1-(propionyloxy)propoxy)(4-(phenyl-d5)butyl-4,4-d2)phosphoryl)acetyl)pyrrolidine-2-carboxylate, monosodium salt
Synonyms:
Molecular weight: 592.7
CAS: 1217819-83-4
Purity: ≥99% deuterated forms (d1-d7)
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 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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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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