Silodosin-d4 is intended for use as an internal standard for the quantification of silodosin (Item No. 14866) by GC- or LC-MS. Silodosin is an α1A-adrenergic receptor (α1A-AR) antagonist (Ki = 0.036 nM).{25007} It is 583- and 56-fold selective for α1A- over α1B- and α1D-ARs, respectively. Silodosin inhibits phenylephrine-induced contraction of isolated rabbit prostate (pA2 = 10.05) more potently than rabbit or rat aorta (pA2s = 9.36 and 8.13, respectively).{55032} It inhibits norepinephrine-induced contraction of isolated human prostate tissue when used at concentrations ranging from 0.3 to 10 nM.{25007} Silodosin (0.01-1,000 µg/kg) inhibits phenylephrine-induced increases in intraurethral pressure in rats.{25005} Formulations containing silodosin have been used in the treatment of benign prostatic hyperplasia.
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An internal standard for the quantification of silodosin by GC- or LC-MS
Formal name: (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl-1,1,2,2-d4)amino)propyl)indoline-7-carboxamide
Synonyms: KMD-3213-d4
Molecular weight: 499.6
CAS: 1426173-86-5
Purity: ≥99% deuterated forms (d1-d4)
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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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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The tetracycline repressor (TetR) is a transcriptional regulator which normally binds tightly to its palindromic tetO operator DNA, blocking gene expression.{17508} Tet causes the repressor to dissociate from the DNA, allowing transcription to occur. A novel reverse TetR (revTetR) requires tetracycline as a co-repressor to bind tetO and block transcription.{17509,17510} Anhydrotetracycline (hydrochloride) is a powerful effector in both the tetracycline repressor (TetR) and reverse TetR (revTetR) systems, binding the Tet repressor 35-fold more strongly than Tet.{17508,17511} Moreover, anhydrotetracycline poorly binds the 30S ribosomal subunit, compared to Tet,{17512} so it does not act as a general inhibitor of translation and is a poor antibiotic. Perhaps related to this, the concentration of anhydrotetracycline that inhibits eukaryotic cell growth is more than a 1,000-fold above the dose that alters transcription through TetR.{17508}
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