Growth hormone releasing factor (GRF) stimulates pituitary somatotropin (ST) release. Somatotropin directly or indirectly through insulin like-growth factor I decreases lipogenesis and promotes protein accretion resulting in enhanced growth in food producing animals such as cattle and swine. A s...
Growth hormone-releasing factor is the main endogenous stimulator of somatotropin secretion. Our objective was to compare the effects of recombinant growth hormone-releasing factor and recombinant bST on somatotropin secretion, mammary function, and body composition of lactating, primiparous dai...
Our objective was to compare the effects of recombinant bovine growth hormone-releasing factor and recombinant bST on the somatotropic cascade in lactating dairy cows. Primiparous cows were killed after 63 d of continuous daily infusion with 12 mg of releasing factor or 29 mg of bST or no infusi...
We examined the effect of the two protein tyrosine kinase inhibitors, α-cyano-3-ethoxy-4-hydroxy-5-phenylthiomethylcinnamide (ST638) and herbimycin A, on the activation processes of rat basophilic leukemia (RBL-2H3) cells by cross-linking of IgE receptors. RBL-2H3 cells sensitized with DNP-spec...
In order to investigate the biochemical nature of intracellular cascades leading to cellular differentiation in vitro, we examined the effect of inhibitors of protein phosphorylation on terminal erythroid differentiation of mouse erythroleukemia (MEL) cells. We have found that specific inhibitor...
We have investigated the involvement of protein-tyrosine kinases in thrombin-induced aggregation of human platelets, using ST638 and genistein which are known inhibitors of protein-tyrosine kinase. Preincubation of platelets with 50 μM of ST638 or 25 μg/ml of genistein completely blocked the p...
Combining the specificity of radioimmunoscintigraphy and the high sensitivity of PET in an in vivo detection technique could improve the quality of nuclear diagnostics. Positron-emitting nuclide 76Br (T1/2=16.2 h) might be a possible candidate for labeling monoclonal antibodies (mAbs) and their ...
Two methods were investigated for the no-carrier-added synthesis of N-succinimidyl 4-[18F]fluorobenzoate (S[18F]FB). The first, an attempted nucleophilic aromatic substitution by [18F]fluoride on N-succinimidyl 4-nitrobenzoate was unsuccessful. The second method involved three steps; [18F]fluori...
The preparation of N-succinimidyl-4-[131I]iodobenzoate (SIB) has been optimized using an alternative technique employing Cu(I)-assisted radioiododebromination that produces p-[131I]iodobenzoic acid. The reaction conditions were optimized and radiochemical purity of more than 90% was obtained whe...
IntroductionAlpha particles are radiation of high energy and short range, properties that can lead to radiolysis-mediated complications in labeling chemistry at the high radioactivity levels required for clinical application. In previous papers in this series, we have shown that radiation dose h...
Monoclonal antibody 38S1 was radiobrominated with the positron emitter 76Br (T1/2 = 16.2 h). Indirect labeling was performed using N-succinimidyl para-(tri-methylstannyl)benzoate (SPMB) as the precursor molecule. SPMB was labeled using Chloramine-T yielding N-succinimidyl para-[76Br]bromobenzoat...
A new method is reported for the synthesis of N-succinimidyl p-([125127I]iodobenzoate (NS-p-IB) from N-succinimidyl p-(tri-n-butylstannyl)benzoate via an iodination-destannylation reaction. The tin precursor was obtained in 70% overall yield from p-bromobenzoyl chloride after a four-step synthes...
Lithium 2,4-dimethoxy-3-lithiobenzoate can be efficiently generated from 2,4-dimethoxy-3-bromobenzoic acid in THF at −100°C.
N-succinimidyl-3-(tri-n-butylstannyl)benzoate (m-BuATE), N-succinimidyl-3-(tri-methylstannyl)benzoate (m-MeATE) and N-succinimidyl-4-(tri-n-butylstannyl)benzoate (p-BuATE) were synthesized and radioiodinated using either N-chlorosuccinimide (NCS) or t-butylhydroperoxide (TBHP) as the oxidant. Ra...
A method is described for labeling proteins with 7.2 h half-life 211At. The α particle-emitting nuclide was coupled to goat IgG using an N-succinimidyl 3-(tri-n-butylstannyl) benzoate intermediate. The reaction and purification sequence requires about 2 h to produce 211At-labeled IgG in 25–40%...
N-Succinimidyl 4-methyl-3-(tri-n-butylstannyl)benzoate (MATE) was synthesized in two steps from 4-methyl-3-iodobenzoic acid. Radioiododestannylation of MATE proceeded more slowly than N-succinimidyl 3-(tri-n-butylstannyl)benzoate (ATE), but for reaction periods of 10 min or more, identical yield...
The relative affinity and selectivity of the stereoisomers of 3-quinuclidinyl atrolactate (QNA) and the enantiomers of 3-quinuclidinyl xanthene-9-carboxylate (QNX) for the pharmacologically defined muscarinic receptor subtypes was determined using functional responses of rabbit vas deferens (M1)...
Five new di-Schiff base nickel(II) complexes (1–5) of salen type ligands were synthesized in-situ by condensation of 3-(dimethylamino)-1-propylamine with 2-hydroxybenzaldehyde, 2-hydroxy-5-methyl benzaldehyde, 2-hydroxy-5-bromo benzaldehyde, 2-hydroxy-5-nitrobenzaldehyde and 2-hydroxy-1-naphtha...
Biodiesel, an environment friendly alternative for fuels, contains methyl esters of long-chain fatty acids. Our group has reported a methanol-stable YLIP9 from Yarrowia lipolytica MSR80 that shows poor catalysis of long-chain fatty acids. To shift its substrate specificity, residues within lid a...
Engineering a methanol tolerant lipase is of great importance in biodiesel production. Here, the first semi-rational method for directed enzyme evolution to enhance methanol tolerance by targeting high B-factor residues for iterative saturation mutagenesis (ISM) is reported. The best double muta...
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