Norgestimate-d6 is intended for use as an internal standard for the quantification of norgestimate (Item No. 16547) by GC- or LC-MS. Norgestimate is a progestin and a prodrug form of norelgestromin and levonorgestrel (Item No. 10006318).{53982,12452} It binds to progestin receptors (mean IC50 = 3.48 nM for rabbit uterine receptors) and is selective for progestin over androgen receptors (mean IC50 = 764 nM for rat prostatic receptors) in radioligand binding assays.{53983} Norgestimate maintains pregnancy in ovariectomized female rats in a dose-dependent manner.{53982} It inhibits ovulation in 100% of female rats when administered at a dose of 0.5 mg/kg. Norgestimate (2 mg/kg) completely inhibits estrone-induced vaginal cornification in ovariectomized female rats, indicating antiestrogenic activity. Formulations containing norgestimate in combination with ethinyl estradiol have been used as oral contraceptives and in the treatment of acne vulgaris.
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An internal standard for the quantification of norgestimate by GC- or LC-MS
Formal name: (17α)-17-(acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one-2,2,4,6,6,10-d6, 3-oxime
Synonyms: Dexnorgestrel acetime-d6
Molecular weight: 375.5
CAS: 1263194-12-2
Purity: ≥99% deuterated forms (d1-d6)
Formulation: A solid
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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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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