(±)-Felodipine-d5 is intended for use as an internal standard for the quantification of (±)-felodipine (Item No. 17535) by GC- or LC-MS. (±)-Felodipine is an inhibitor of L-type calcium channels.{28544} It induces relaxation of precontracted isolated porcine coronary artery segments (EC50 = 0.15 nM), which highly express L-type calcium channels.{53284} (±)-Felodipine is selective for L-type calcium channels over N-, R-, and P/Q-type channels at 10 µM, as well as the T-type Cav3.2 channel (IC50 = 6.8 µM).{28544,28732} (±)-Felodipine preferentially inhibits L-type calcium channels in isolated rat portal vein over rat left ventricle (IC50s = 33.9 and 3,981 nM, respectively).{28545} It decreases mean arterial blood pressure and total peripheral resistance in a rabbit model of hypertension induced by renal artery ligation when administered intravenously at doses of 30 and 100 nmol/kg.{53285}
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An internal standard for the quantification of (±)-felodipine by GC- or LC-MS
Formal name: 4-(2,3-dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid, 3-(ethyl-d5) 5-methyl ester
Synonyms:
Molecular weight: 389.3
CAS: 1242281-38-4
Purity: ≥99% deuterated forms (d1-d5)
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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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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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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