| Description | CYTL1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYTL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control. Components CYTL1 siRNA-1: 5 nmol (HPLC) CYTL1 siRNA-2: 5 nmol (HPLC) CYTL1 siRNA-3: 5 nmol (HPLC) siRNA Negative Control:CYTL1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYTL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control. Components CYTL1 siRNA-1: 5 nmol (HPLC) CYTL1 siRNA-2: 5 nmol (HPLC) CYTL1 siRNA-3: 5 nmol (HPLC) siRNA Negative Control: 5 nmol (HPLC) FAM-labeled siRNA Negative Control: 5 nmol (HPLC) GAPDH siRNA Positive Control:5 nmol (HPLC)... Read More | Proteinase K is a stable and highly reactive serine protease. Evidence from crystal and molecular structure studies indicates the enzyme belongs to the subtilisin family with an active-site catalytic triad (Asp39-His69-Ser224). It is stable in a broad range of environments: pH, buffer salts, Proteinase K is a stable and highly reactive serine protease. Evidence from crystal and molecular structure studies indicates the enzyme belongs to the subtilisin family with an active-site catalytic triad (Asp39-His69-Ser224). It is stable in a broad range of environments: pH, buffer salts, detergents (SDS), and temperature. In the presence of 0.1-0.5% SDS, proteinase K retains activity and will digest a variety of proteins and nucleases in DNA preparations without compromising the integrity of the isolated DNA.ApplicationUseful for the proteolytic inactivation of nucleases during the isolation of DNA and RNA.Removes endotoxins that bind to cationic proteins such as lysozyme and ribonuclease A.Reported useful for the isolation of hepatic, yeast, and mung bean mitochondriaDetermination of enzyme localization on membranesTreatment of paraffin embedded tissue sections to expose antigen binding sites for antibody labeling.Digestion of proteins from brain tissue samples for prions in Transmissible Spongiform Encephalopathies (TSE) research... Read More | Purity: >95%, by SDS-PAGE visualized with Coomassie® Blue Staining. Description:Cyclophilin B (SCYLP, CyPB, and peptidyl-prolyl cis-trans isomerase B) is a 24 kDa glycoprotein member of the B subfamily of the cyclophilin-type PPIase family of molecules. It is both secreted and retained in Purity: >95%, by SDS-PAGE visualized with Coomassie® Blue Staining. Description:Cyclophilin B (SCYLP, CyPB, and peptidyl-prolyl cis-trans isomerase B) is a 24 kDa glycoprotein member of the B subfamily of the cyclophilin-type PPIase family of molecules. It is both secreted and retained in the ER. When secreted, it mediates chemotaxis and T cell adhesion to fibronectin. This is likely due to its prolyl cis/trans isomerase activity. Intracellularly, Cyclophilin B appears to serve as a molecular chaperone for molecules destined for secretion. It does so via stabilization and facilitating the activity of additional chaperones. The human CyPB precursor is 216 amino acids (aa) in length. It contains a 25 aa signal sequence plus a 191 aa mature region. There is a partial heparin-binding sequence (aa 27‑34), a PPIase domain (aa 47‑204), and a C-terminal ER retention motif (aa 213‑216). Over aa 34‑216, the human and mouse sequences are 95% aa identical... Read More | Inquire | Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C ( 5-HT 2C ) receptor -selective agonist with an EC 50 of 8 nM.In VitroVabicaserin displaces 125 I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT 2C receptor sites in Chinese hamster ovary cell membranes with a K i value of 3 nM and Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C ( 5-HT 2C ) receptor -selective agonist with an EC 50 of 8 nM.In VitroVabicaserin displaces 125 I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT 2C receptor sites in Chinese hamster ovary cell membranes with a K i value of 3 nM and is >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors. Binding affinity determined for the human 5-HT 2B receptor subtype using [ 3 H]5HT is 14 nM. Vabicaserin is a potent and full agonist (EC 50, 8 nM; E max, 100%) in stimulating 5-HT 2C receptor-coupled calcium mobilization and exhibits 5-HT 2A receptor antagonism and 5-HT 2B antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression. Vabicaserin exhibits lower affinity at the 5-HT 2C antagonist binding site (22 nM) labeled with [ 3 H]mesulergine. Additional binding studies indicate that Vabicaserin possesses affinity for the 5-HT 2B and 5-HT 1A receptors with K i values of 14 and 112 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAfter a single oral dose of [ 14 C]Vabicaserin at 50, 5, and 15 mg/kg, unchanged drug represents less than 19, 20, and 35% of total plasma radioactivity at all the time points examined in mice, rats, and dogs, respectively. The carbamoyl glucuronide (CG) represents approximately 7 to 36% of plasma radioactivity in mice and 2 to 28% of plasma radioactivity in dogs but is not detected in rat plasma after the single [ 14 C]Vabicaserin dose. However, the CG is observed in rat plasma after multiple-dose administration of Vabicaserin at higher doses, and the CG is approximately 20 times less than Vabicaserin based on steady-state AUC 0-24 values. The estimated plasma AUC 0-24 ratios of CG to the parent drug are 1.5 and 1.7 in mice and dogs after the single [ 14 C]Vabicaserin dose, respectively. The plasma AUC 0-24 ratios for the CG to Vabicaserin at steady state with doses used for safety assessment are less for mice (0.2-0.6) and slightly higher for dogs (1.8-4.0) compared with the single dose values. The CG is detected in dog urine in similar amounts to the parent drug, although it is not detected in mouse or rat urine after the single [ 14 C]Vabicaserin dose. Radioactivity in a 0- to 24-h bile collection from rats receiving a 5 mg/kg [ 14 C]Vabicaserin dose accounts for 19 and 24% of the administered dose in males and females, respectively. Although the CG is not detected in urine or feces of rats after a single oral administration, it represents an average of up to 30% of biliary radioactivity in male rats and 15% in female rats. In monkeys after a single oral 25-mg/kg dose of Vabicaserin, the plasma concentrations of the CG exceeded those of Vabicaserin at all the time points (2-24 h) postdose, although the amount of CG relative to Vabicaserin decreased by 24 h postdose, with ratios of 17.5 at 2 h and 1.7 at 24 h. The CG to Vabicaserin AUC 0-24 ratio of 12:1 indicates that the CG is a major metabolite in monkeys. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal administrationMice and Rats For metabolism studies in mice, rats, and dogs, radiolabeled doses are used. Male and female CD-1 mice and Sprague-Dawley rats are used. The dose vehicle for mice and rats contained 2% (w/w) Tween 80 and 0.5% methylcellulose in water. Nonfasted male and female mice weighing from 27.8 to 33.8 g at the time of dosing are given a single 50-mg/kg (∼300 µCi/kg) dose of Vabicaserin at a volume of 20 mL/kg via intragastric gavage. Mice are kept in metabolic cages in groups of five. Nonfasted male rats weighing from 318 to 345 g and female rats weighing from 227 to 255 g at the time of dosing are given a single 5-mg/kg (∼300 µCi/kg) dose of Vabicaserin at a volume of 2.5 mL/kg via intragastric gavage. Four bile duct-cannulated male rats weighing from 387 to 411 g and four bile duct-cannulated female rats weighing from 291 to 325 g at the time of dosing are nonfasted and are given a single 5-mg/kg (323 µCi/kg) dose of Vabicaserin at a volume of 5.0 mL/kg via intragastric gavage. Rats are kept individually in metabolism cages. Dogs Four male beagle dogs, weighing from 7.6 to 9.8 kg at the time of dosing, are from an in-house colony. Approximately 11 mg of [ 14 C]Vabicaserin hydrochloride and 940 mg of nonlabeled Vabicaserin hydrochloride are dissolved in methanol and then evaporated under a nitrogen stream to dryness. Capsules (number 2) are filled with accurate amounts (126.7-138.1 mg) of the mixed drug substance according to animal weights to give a dosage of 15 mg/kg (39 µCi/kg). The filled gelatin capsules are then enteric-coated manually. Each dog is given one enteric-coated capsule containing [ 14 C]Vabicaserin as the hydrochloride salt. Animals are fed 2 h before dosing and are housed individually in metabolic cages. Monkey Four male cynomolgus monkeys, weighing from 5.4 to 9.6 kg at the time of dosing, are from an in-house colony. Nonfasted monkeys are given a single 25-mg/kg dose of nonradiolabeled Vabicaserin at a volume of 2 mL/kg via intragastric gavage. The vehicle is the same as used in mice and rats. Animals are housed individually in metabolic cages. aladdin has not independently confirmed the accuracy of these methods. They are for reference only.IC50& Target:5-HT 2C Receptor 8 nM (EC 50 )... Read More |