Prazosin-d8 is intended for use as an internal standard for the quantification of prazosin (Item No. 15023) by GC- or LC-MS. Prazosin is an antagonist of α1-adrenergic receptors (α1-ARs).{22637,22636} It selectively binds to α1-ARs with Ki values of 0.2, 0.25, and 0.32 nM for the human recombinant α1A-, α1B-, and α1D-ARs, respectively, over α2-ARs (Kis = 340 and 3.7 nM in α2A-AR-expressing HT-29 cells and α2B-AR-expressing NG108 cells, respectively).{29094,46466} It also binds to melatonin receptor 3 (MT3) in hamster brain membranes (IC50 = 7.8 nM).{22638} Prazosin inhibits peripheral and central postsynaptic α1-ARs with IC50 values of 0.2 and 1.7 nM in isolated dog aorta and rat brain, respectively.{22637} It decreases diastolic blood pressure in normal, renal hypertensive, and spontaneously hypertensive rats when administered at a dose of 1 mg/kg.{46467} Prazosin (1.5 mg/kg) increases the number of entries and percentage of time spent in the open arms of the elevated plus maze, indicating anxiolytic-like activity, in alcohol-consuming rats and also reduces alcohol intake and alcohol-seeking behavior in alcohol-preferring rats.{46468,46469}
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An internal standard for the quantification of prazosin by GC- or LC-MS
Formal name: [4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl-2,2,3,3,5,5,6,6-d8]-2-furanyl-methanone
Synonyms:
Molecular weight: 391.5
CAS: 1006717-55-0
Purity: ≥99% deuterated forms (d1-d8)
Formulation: A solid
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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The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
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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 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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