42results about How to "High labeling yield" patented technology

Methods and apparatus enable radiosynthesis of radiolabeled compounds using electrochemical trapping and release. The trapping and release of radioactive isotopes all occur inside a microreactor, a vial or similar device, thus eliminating the need for azeotropic drying and several dead-end filling steps, as well as the necessity to move concentrated radioisotopes from one compartment of the chip to another. These and other features allow radioisotope enrichment to be carried out internally within a radiochemical synthesis chip, providing faster and more robust operation, as well as producing very high radiochemical labeling yields.

The invention provides an RGD polypeptide coordination complex of a radioactive nuclide label. According to the structure of the coordination complex, the radioactive nuclide is selected from 64Cu, 68Ga, 111In, 62Cu, 67Cu, 67Ga, 86Y, 89Zr or 18F; the ligand is a ligand compound containing an RGD structure, which is shown in a formula (I). The coordination complex has stronger ligand stability and high target/non-target ratio, and the appetency of the ligand with integrin AlphavBeta3 is stronger. The invention further provides a preparation method of the coordination complex, and an application of the coordination complex in preparing tumor developers.

The invention discloses a [<18>F] AlF marked positron emission tomography (PET) polypeptide probe and a preparation method thereof. The probe comprises TMTP1 polypeptide and NOTA, which are connected together, and the structural formulae of the TMTP1 polypeptide and the NOTA are shown in the description. According to the [<18>F] AlF marked positron emission tomography (PET) polypeptide probe and the preparation method thereof, a glycine is added to the TMTP1, and a G-TMTP1 polypeptide is designed, so that the polypeptide does not influence the biological activity after being radioactively marked; furthermore, 18F is taken as a radionuclide, and the G-TMTP1 polypeptide is marked by utilizing a [<18>F] AlF-NOTA method, so that the obtained [<18>F] AlF-marked PET polypeptide probe has excellent pharmacokinetics properties, the background cleaning rate is high, the liver uptake rate is low, in-vivo stability is good, the uptake rate of tumor site is high, highly metastatic tumor can be diagnosed specifically, and the polypeptide probe can be applied to diagnosis or therapeutic evaluation of highly metastatic malignant tumor.

The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the genera formula (I) wherein: R is (C₁-C₆) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1-6; and m=0 or 1; and X is a halogen atom. The invention further relates to precursor compounds for these analogues, to a method of preparing these analogues, to a pharmaceutical composition comprising these analogues and to the use of these analogues and compositions in the diagnosis of cancer.

The present invention is linked inheritance mapping method utilizing SRAP molecular mark for cotton. The mapping population is hybridization between sea island cotton and upland cotton to generate F2 single plant. Applying SRAP molecular mark and PCR proliferation for detecting population polymorphism in inheritance mapping obtains 285 polymorphic bands in high yield. The 285 marks are used in constructing MAPMAKER linkage group, and 237 marks enter 39 linkage groups, each of which has 2-13 marks. All the linkage groups have the total length of 3030.7 cM, covers 65.4 % of the total cotton genome, and the average mark interval is 12.79 cM. The marks are distributed in the linkage groups relatively homogeneously. The specific molecule marking steps and electrophoresis parameters are also proposed.

The invention belongs to the technical field of fluorescence in situ hybridization, and in particular relates to a ready-to-use multi-probe hybridization glass slide and a preparation method and application thereof. The multi-probe hybridization slide is composed of a probe attachment slide, each probe, a hybridization buffer and a sample attachment slide; each probe is respectively attached to each independent probe attachment area in a freeze-dried form; The sample is dropped on the sample attachment area, and when the sample attachment area and the probe attachment area are attached, the sample in the sample attachment area is hybridized with the probe in the corresponding probe attachment area. Compared with the traditional FISH experiment, the present invention can simultaneously preset multiple groups of probes on one glass slide, and can complete the detection of various probes on the same slide, greatly simplifying the operation steps of traditional FISH; The usage amount of the probe reduces the usage cost of the probe; the ready-to-use multi-probe hybridization glass slide of the present invention has extremely high signal-to-noise ratio, specificity and sample detection rate.

The invention discloses a technetium-99m-labeled graphene oxide nanoparticle and a preparation method thereof. The preparation method comprises the steps as follows: (1) enabling an alkynyl-modified ligand compound and azido-modified graphene oxide to have a Click reaction, and purifying coarse products to obtain a reactant A, wherein the ligand compound is a macrocyclic ligand compound; (2) evenly mixing the reactant A, a hydrochloric acid of stannous chloride and high-technetium acid radial ions in a solvent to obtain mixed liquor, adjusting the pH of the mixed liquor to 6.0-7.5, and performing a reduction coordination reaction to obtain the nanoparticle. The preparation method is high in reaction selectivity, mild in condition, simple to operate and higher in labeling yield. The technetium-99m-labeled graphene oxide nanoparticle is very good in biocompatibility and better in water solubility, can be used for studying the real-time distribution condition of graphene oxide in the cell level and the small animal level and provides more basic information for the application of the graphene oxide to organisms later.

The present invention relates to a labeling method for a hydroxytamine transporter imaging agent [<18>F]-FPBM. According to the method, a <18>F labeling treatment is performed on 1,3-di-p-toluenesulfonyl propane; the resulting labeled intermediate 1-fluoro(<18>F)-3-p-toluenesulfonyl propane reacts with 2-aminobenzene-(2-(N,N-dimethyl)-4-hydroxy)-phenylsulfide to obtain the [<18>F]-FPBM, wherein the reaction process is represented by the following. According to the present invention, the precursor compound 2-aminobenzene-(2-(N,N-dimethyl)-4-hydroxy)-phenylsulfide is firstly used for label of the FPBM, the results show that the compound provides good selectivity for the small molecular chain linking reaction, and the total labeling yield of the labeling method is 13-25%. With the present invention, the optimization of the radioactive synthesis process of the compound is solved, the labeling yield is improved, the automation synthesis is firstly achieved, and the basis is established for the clinical application of the [<18>F]-FPBM in the future.

The invention provides a dimeric amido benzimidazole compound. The structure of the dimeric amido benzimidazole compound is shown as a formula (I), wherein R0 is an integer of n from 0 to 5. The invention also provides a compound with anti-tumor activity and a radionuclide labeled compound targeted by interferon stimulating protein, wherein the compound is based on the dimeric amido benzimidazole compound. The dimeric amido benzimidazole compound has high affinity and high specificity to interferon stimulating protein, the compound with anti-tumor activity has the characteristic of activating an STING pathway in vitro, and the radionuclide labeled compound has the advantages that target uptake and non-target uptake are obviously compared, and the lipid solubility can be changed by introducing nuclides with different properties so that the application scene is greatly widened, and the compound can be combined with treatment nuclides for tumor treatment, and even can be used for immunotherapy.

A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [¹²³Iodine](R)—N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([¹²³I]MIPP) with a leaving group Bu₃Sn.

The invention relates to a method for radiolabeling a biological compound. The method comprises the following steps of performing chelation reaction on a bifunctional chelating agent modified with a maleimide group and radionuclide, and directly adding the biological compound to carry out coupling reaction, thereby obtaining the radiolabeled biological compound. The technical scheme adopts the maleimide group with excellent thermal stability, so that the bifunctional chelating agent can be chelated with radioactive metal ions under a high-temperature condition, the chelating reaction time is remarkably shortened, and the labeling efficiency is improved; and the product of the chelation reaction can be subjected to biological compound coupling without purification, and the method has the advantages of simple steps, convenience, high efficiency and high connection efficiency.

There is provided a method for preparing a ^99mTc labeled gold nanoparticles-gold binding peptide, including: (a) coating gold nanoparticles with a gold binding peptide; and (b) labeling a composed ^99mTc tricarbonyl precursor on the gold binding peptide coated on the gold nanoparticles. The ^99mTc labeled gold nanoparticles-gold binding peptide prepared by the method according to the present invention is expected to be usefully employed for manufacturing a molecular contrast agent (imaging agent) which is traceable in organisms using imaging apparatuses such as gamma imaging and single photon emission computed tomography due to high labeling yield and good in-vivo stability.

The invention relates to the technical field of stable isotope labeling, in particular to a stable isotope amino compound labeling reagent and a synthesis method and application thereof. The chemical structural formula of the labeling reagent is as shown in formula 1 in the specification, wherein in the formula 1, X is D, and the labeling reagent is [d4]-2-(9-acridone)-ethyl chloroformate; and R is any one of F, Cl, Br, I and other elements, and n is equal to 2 or 3. The isotope labeling reagent provided by the invention takes acridone as a parent ring and an isotope labeling group and chloroformate as a reaction group, can selectively label an amino compound, and has the advantages of simple and convenient synthesis method, high labeling reaction rate, strong signal of a labeled product, high labeling yield and high amino selectivity; and the accuracy and the sensitivity of mass spectrometric detection of the amino compound are enhanced.

The invention discloses a [18F] DPA-174 derivative. The [18F] DPA-174 derivative is prepared by modifying the benzene ring structure of or prolonging the carbon chain structure of a [18]F DPA-174 imaging agent. The invention also discloses preparation and application methods of the [18F] DPA-174 derivative. The [18F] DPA-174 derivative is simple in preparation, easy to implement, high in labellingyield and good in repeatability and can help in real time observe and in vivo monitor the status of intracerebral neuroinflammation of an animal model as well as the changes of the major organs and tissues of the animal model; the prepared imaging agents can achieve imaging effects on neuroinflammation; the [18F] DPAF imaging agent can achieve a high signal-to-noise ratio on neuroinflammation lesions to provide possibility for further monitoring and assessing the diagnosis and treatment effects on neuroinflammation..

New methodologies for site-specifically radiolabeling proteins with the PET isotope [^1SF] are required to generate high quality radiotracers for imaging in both the preclinical and clinical settings. The enzymatic radiofluorination overcomes many of the limitations encountered to date with purely chemical approaches. The bacterial enzyme lipoic acid ligase was used to conjugate [¹⁸F]-fluorooctanoic acid to both a small peptide and a Fab antibody fragment. Labeling was site-specific and highly efficient under mild aqueous conditions using small amounts of peptide/protein (1-10 nmol). The labeled construct retained full epitope binding affinity and was stable in mouse serum. Using an optimized reaction scheme, mCi quantities of [¹⁸F]-Fab were generated, an amount sufficient for human imaging.