Vortioxetine-d8 is intended for use as an internal standard for the quantification of vortioxetine (Item No. 23694) by GC- or LC-MS. Vortioxetine is a multimodal serotonergic agent that acts as a serotonin (5-HT; Item No. 14332) reuptake inhibitor (Ki = 1.6 nM) and binds to the 5-HT1A, 5-HT1B, 5-HT3A, and 5-HT7 receptors (Kis = 15, 33, 3.7, and 19 nM, respectively).{36248} It also binds to the β1-adrenergic receptor (Ki = 46 nM). It acts as an antagonist at 5-HT3A and 5-HT7, a partial agonist at 5-HT1B, and a full agonist at 5-HT1A receptors. Vortioxetine is selective for the serotonin transporter (SERT) over the dopamine and norepinephrine transporters (IC50s = 5.3, 890, and 140 nM, respectively). It has affinity for histamine H2, melanocortin 4, β2-adrenergic, 5-HT2C, and 5-HT6 receptors with Ki values greater than 180 nM, but it is selective over the majority of targets in a panel of 75 ion channels, G protein-coupled receptors, enzymes, and transporters. Vortioxetine (5 or 10 mg/kg per day) increases 5-HT levels in vivo in rat brain and decreases occupancy at SERT. At acute and chronic doses of 5 mg/kg, but not 10 mg/kg, it increases the time mice spend in the center of the open field test, increases mobility in the forced swim test, and decreases the latency to feed in the novelty suppressed feeding test.{36249} It also increases proliferation and survival of adult-born granule cells in the hippocampus. Formulations containing vortioxetine have been used in the treatment of major depressive disorder.
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An internal standard for the quantification of vortioxetine by GC- or LC-MS
Formal name: 1-(2-((2,4-dimethylphenyl)thio)phenyl)piperazine-2,2,3,3,5,5,6,6-d8
Synonyms:
Molecular weight: 306.5
CAS: 2140316-62-5
Purity: ≥99% deuterated forms (d1-d8)
Formulation: A solid
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 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}
Available on backorder
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}
Available on backorder