Cariprazine-d6 is intended for use as an internal standard for the quantification of cariprazine (Item Nos. 31446 | 24025) by GC- or LC-MS. Cariprazine is an atypical antipsychotic.{60050} It binds to dopamine D2L, D2S, and D3 receptors, the serotonin (5-HT) receptor subtypes 5-HT1A, 5-HT2A, and 5-HT2B, and histamine H1 and sigma-1 (σ1) receptors (Kis = 0.085-23.44 nM).{36514} Cariprazine is an antagonist of dopamine D2 and D3 receptors (Kbs = 0.759 and 0.316 nM, respectively, in dopamine-induced [35S]GTPγS binding assays). It is also a partial agonist at these receptors, stimulating inositol phosphate production in murine A9 cells expressing human D2L receptors (EC50 = 3.16 nM) and inhibiting forskolin-induced cAMP accumulation in CHO cells expressing human D3 receptors (EC50 = 2.63 nM). Cariprazine inhibits amphetamine-induced hyperactivity and the conditioned avoidance response in rats (ED50s = 0.12 and 0.84 mg/kg, respectively).{60051} It also inhibits scopolamine-induced learning deficits in a water labyrinth learning test in rats when administered at doses ranging from 0.02 to 0.08 mg/kg. Formulations containing cariprazine have been used in the treatment of schizophrenia, as well as manic, depressive, or mixed episodes associated with bipolar I disorder.
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An internal standard for the quantification of cariprazine by GC- or LC-MS
Formal name: N’-[trans-4-[2-[4-(2,3-dichlorophenyl)-1-piperazinyl]ethyl]cyclohexyl]-N,N-di(methyl-d3)-urea
Synonyms:
Molecular weight: 433.5
CAS: 1308278-67-2
Purity: ≥99% deuterated forms (d1-d6)
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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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 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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