Ziprasidone-d8 is intended for use as an internal standard for the quantification of ziprasidone (Item No. 15031) by GC- or LC-MS. Ziprasidone is an atypical antipsychotic.{26444} It is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (EC50 = 36.31 nM for inhibition of forskolin-induced adenylate cyclase activity in HeLa cells expressing human receptors), as well as an inverse agonist of 5-HT1D receptors (IC50 = 2.69 nM) and a partial agonist of 5-HT1B receptors (EC50 = 6.17 nM) in [35S]GTPγS binding assays.{54360,22640} Ziprasidone is an antagonist at 5-HT2A and dopamine D2 receptors (Kis = 1.15 and 1.29 nM, respectively) in cell-based assays.{54361} It inhibits d-amphetamine-induced hyperactivity and apomorphine-induced stereotypy in rats (ID50s = 1.53 and 2.43 mg/kg, respectively). Formulations containing ziprasidone have been used in the treatment of schizophrenia and bipolar I disorder.
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An internal standard for the quantification of ziprasidone by GC- or LC-MS
Formal name: 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl-2,2,3,3,5,5,6,6-d8]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one
Synonyms: CP-88,059-d8
Molecular weight: 421
CAS: 1126745-58-1
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 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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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 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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