Dronedarone-d6 is intended for use as an internal standard for the quantification of dronedarone (Item No. 9000543) by GC- or LC-MS. Dronedarone is an antiarrhythmic agent and a derivative of amiodarone (Item No. 15213).{41032,41033} It inhibits muscarinic acetylcholine receptor-dependent potassium currents induced by carbachol (carbamoylcholine; Item No. 14486) or intracellular loading of GTPγS in single cells isolated from guinea pig atria (IC50s = 0.1 and 1 µM, respectively).{41033} Dronedarone (50 and 100 mg/kg) reduces sinus frequency and prolongs action potential duration (APD) in isolated rabbit ventricular myocardium. It increases atrial APD and the atrial effective refractory period (AERP) in a dog model of atrial fibrillation induced by rapid right atrial pacing.{57286} Formulations containing dronedarone have been used in the treatment of atrial fibrillation.
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An internal standard for the quantification of dronedarone by GC- or LC-MS
Formal name: N-[2-butyl-3-[4-[3-(dibutylamino)propoxy-1,1,2,2,3,3-d6]benzoyl]-5-benzofuranyl]-methanesulfonamide, monohydrochloride
Synonyms:
Molecular weight: 599.3
CAS: 1329809-23-5
Purity: ≥99% deuterated forms (d1-d6)
Formulation: A solid
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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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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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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