Rofecoxib-d5 is intended for use as an internal standard for the quantification of rofecoxib (Item No. 10010260) by GC- or LC-MS. Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
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An internal standard for the quantification of rofecoxib by GC- or LC-MS
Formal name: 4-[4-(methylsulfonyl)phenyl]-3-(phenyl-d5)-2(5H)-furanone
Synonyms:
Molecular weight: 319.4
CAS: 544684-93-7
Purity: ≥99% deuterated forms (d1-d5)
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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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 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.
Available on backorder