Clonidine-d4 is intended for use as an internal standard for the quantification of clonidine (Item No. 15949) by GC- or LC-MS. Clonidine is an agonist of α2-adrenergic receptors (α2-ARs; Kis = 61.66, 69.18, and 134.9 nM for α2A-, α2B-, and α2C-ARs, respectively).{40326} It stimulates [35S]GTPγS binding to HEK293 cell membranes expressing the human receptors with EC50 values of 26.92, 56.23, and 912.01 nM for α2A-, α2B-, and α2C-ARs, respectively. Clonidine also binds to I1-imidazoline sites in a variety of cell and tissue types (Kds = 4-15 nM).{46373} It induces relaxation of isolated mesenteric artery rings precontracted with norepinephrine (Item No. 16673) when used at a concentration of 10 μM.{25849} Clonidine (10 μM) also induces membrane hyperpolarization and reduces norepinephrine-induced depolarization in isolated mesenteric artery rings. Clonidine (0.1 and 1 μg/kg) reduces mean blood pressure and heart rate when administered via microinjection to the nucleus reticularis lateralis (NRL) of anesthetized normotensive cats.{36359} Formulations containing clonidine have been used in the treatment of hypertension.
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An internal standard for the quantification of clonidine by GC- or LC-MS
Formal name: N-(2,6-dichlorophenyl)-4,5-dihydro-d2-1H-imidazol-4,5-d2-2-amine, monohydrochloride
Synonyms:
Molecular weight: 270.6
CAS: 67151-02-4
Purity: ≥99% deuterated forms (d1-d4)
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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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 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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1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
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