| Description | Extinction Coefficient: 0.7 High Molecular Weight kininogen, synthesized by hepatocytes, is a multifunctional protein. It is the precursor protein of bradykinin. In addition it is a cofactor in the activation of factor XI, XII, and prekallikrein and a major extra-cellular cysteine proteinase Extinction Coefficient: 0.7 High Molecular Weight kininogen, synthesized by hepatocytes, is a multifunctional protein. It is the precursor protein of bradykinin. In addition it is a cofactor in the activation of factor XI, XII, and prekallikrein and a major extra-cellular cysteine proteinase inhibitor. Kininogens inhibit systemic proteases which are thought to have a part in various diseases such as cancer, muscular dystrophy and joint disease. Prepared from plasma shown to be non reactive for HbsAG, anti-HCV, anti-HBc, and negative for anti-HIV 1 & 2 by FDA-required tests... Read More | Product introduction：Used to isolate lymphocytes from human organsMatters needing attention：1. samples, reagents and experimental environment in the whole process shall be carried out at 20 ± 2 ℃. In order to obtain the best experimental results, it is best to carry out the Product introduction：Used to isolate lymphocytes from human organsMatters needing attention：1. samples, reagents and experimental environment in the whole process shall be carried out at 20 ± 2 ℃. In order to obtain the best experimental results, it is best to carry out the experiment within 2 h of sampling. The longer the sample is stored, the worse the cell separation effect is. The separation effect is even worse after the sample is placed for more than 6 h, or even cannot achieve the purpose of separation. 2. in this experiment, it is better not to use plastic products with high polymerization materials (such as polystyrene), but use non-static, low static ionization heart tubes and glass products without alkali treatment, because the electrostatic effect will lead to cell adhesion, and the surface of alkali treated glass will become rough, which will affect the effect of cell separation. 3. aspirating too many lymphocyte layers and separation liquid layers will cause the granulocytes at the junction of separation liquid to be aspirated, thus increasing the number of mixed granulocytes. 4. when the amount of separating solution is greater than that of tissue single cell suspension sample, the separation effect is better.Scope of application：Lymphocyte isolation... Read More | Product Application：KNK437 has been used: as a heat shock factor 1 (HSF1) inhibitor to study its effects on the inhibition of viability and apoptosis activation in chemoresistant mice cells as an HSF1 inhibitor to study its effects on viability and apoptosis of colorectal cancer cells as a Product Application：KNK437 has been used: as a heat shock factor 1 (HSF1) inhibitor to study its effects on the inhibition of viability and apoptosis activation in chemoresistant mice cells as an HSF1 inhibitor to study its effects on viability and apoptosis of colorectal cancer cells as a heat shock protein 70 (HSP70) inhibitor to study its effects on glutamine-induced HSP70 and inflammatory mediator release... Read More | Acid phosphatase is an esterase with broad activity at an optimal pH below 7.0. There are three isozymes, EI, EII, and EIII of similar molecular weight (55 kDa± 5 kDa). Their optimum pH's are 5.5, 4.5, and 4.0 respectively. Acid phosphatase activity was observed by Teller Aladdin Library Acid phosphatase is an esterase with broad activity at an optimal pH below 7.0. There are three isozymes, EI, EII, and EIII of similar molecular weight (55 kDa± 5 kDa). Their optimum pH's are 5.5, 4.5, and 4.0 respectively. Acid phosphatase activity was observed by Teller Aladdin Library Archives in 1954 in preparations of a wheat germ lipase described by Singer JBC, 174, 11, in 1948. Equivalent commercial preparations have been distributed labeled as lipase and acid phosphatase thus generating some confusion. Subsequent work has confirmed that the non-specific esterase activity of the wheat germ preparation may be measured both as lipase (triacetin as substrate) and phosphatase. The enzyme assay is based on the work of Brandenberger and Hanson (Helv. Chim. Acta, 36, 900, 1953) and Hofstee ( Arch. Biochem. Biophys., 51, 239, 1954).Acid phosphatase (APase) non-specifically catalyzes the hydrolysis of monoesters and anhydrides of phosphoric acid to produce inorganic phosphate. It is used to study the production, transport, and recycling of phosphate and the metabolic and energy transduction processes of the cell.Characteristics of Acid Phosphatase from Wheat Germ:Molecular weight: 55,000 ± 5,000 (Verjee 1969).Composition: Three isozymes of closely similar molecular weights have been reported by Verjee (1969): EI, EII, and EIII. See also Brouillard and Ouellet (1965).Optimal pH: EI - 5.5, EII - 4.5, and EIII - 4.0. (Verjee 1969).Specificity: The enzyme has a broad esterase activity. See Joyce and Grisolia (1960). It shows highest activity for pyrophosphate.Inhibitors: Fluoride, molybdate and orthophosphate (Verjee 1969)... Read More | 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 |