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39 results about "CYP1A2" patented technology

Cytochrome P450 1A2 (abbreviated CYP1A2), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. In humans, the CYP1A2 enzyme is encoded by the CYP1A2 gene.

2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and preparation method and application thereof

The invention provides 2, 3, 5, 7-tetrasubstituted dihydro-pyrazolo piperidine derivative and a preparation method and application thereof. The derivative is 2, 3-bis(substituted phenyl)-5-subsituted arylmethyl-7-substituted benzylidene dihydro-pyrazolo piperidine derivative, having the following formula (I). The preparation method includes using substituted arylmethyl amine and methyl acrylate as raw materials; subjecting the materials to Michael addition, Dieckmann condensation and hydrolysis-decarboxylation sequentially; allowing for Aldol reaction with substituted benzaldehyde to obtain intermediate N-substituted arylmethyl-3, 5-bis(substituted benzylidene)-4-piperidone; allowing for condensation with substituted phenylhydrazine to obtain a compound according to the formula (I). The derivative is efficient in inhibiting multiplication of various carcinoma cell lines such as leukemia, esophagus cancer, ovarian cancer and breast cancer in human, is well stably metabolic in liver microsomes of human and rat, is free of direct and competitive inhibition on five enzymes of liver microsomes, such as CYP3A4, CYP2D6, CYP2C9, CYP1A2 and CYP2C19, is highly bioavailable, is low in toxicity to normal cells, and is available for the preparation of drugs for the cancers.
Owner:SHANGHAI NORMAL UNIVERSITY

N-substituted benzyl tetrahydropyridine with indole and preparation method and application thereof

The invention discloses a N-substituted benzyl tetrahydropyridine with -5-substituted indole and preparation method and application thereof, and the structure is shown in the general formula (I): substituted benzene methylamine (ethylamine) and methyl acrylate are raw materials, and an intermediate N-substituted benzylpiperidine (phenylethylpiperidine)-4-ketone is obtained by three steps of reaction such as Michael addition, Dieckmann condensation and hydrolysis decarboxylation or the like in sequence, and the object (I) is obtained by condensation reaction of the intermediate and 5-substituted indole. The compound (I) can effectively inhibit proliferation of human leukemia K562, Jurkat, U937, THP-1 cell line, the human esophagus cancer ECA-109 cell line, human liver cancer SMMC-7721 cell line, human ovary cancer HO-8910 cell line, human breast cancer MCF-7 cell line, breast cancer MDA-MB-231 cell line; the compound has a good metabolism stability in the human and rat liver microsomes; The compound does not have mechanical inhibition effects for five enzymes of human liver microsomes such as CYP3A4, CYP 2D6, CYP2C9, CYP1A2 and CYP2C19 or the like; the compound can induce the cell cycle G2/M retardance and promote cancer cell apoptosis and inhibit cancer cell propagation.
Owner:SHANGHAI NORMAL UNIVERSITY

Gene polymorphism detection kit for guiding psychiatric medication

The invention discloses a gene polymorphism detection kit for guiding psychiatric medication. The kit comprises a specific primer group and a fluorescent probe group, wherein the specific primer group and the fluorescent probe group are used for detecting the rs1065852 site of a CYP2D6 gene, the rs1414334 site of an HTR2C gene, the rs1800497 site of an ANKK1 gene, the rs762551 site of a CYP1A2 gene, the rs489693 site of an MC4R gene and the rs1799978 site of a DRD2 gene. According to the invention, the primer group and the fluorescent probe group are utilized, and the template DNA is specifically amplified by using a fluorescent PCR amplification technology, so that the polymorphism of a plurality of sites of a plurality of genes related to psychotropic drugs can be accurately detected at the same time; ARMS primer design is adopted, mismatched bases are introduced, the specificity of primer amplification is improved, the sensitivity is high, and accurate genotyping can be conducted on human template DNA at the lowest DNA initial amount of 10 ng; the detection speed is high and the efficiency is high: the PCR reaction only needs less than 1 hour to complete the amplification reaction, the cost is lower, the required reagent consumables are all clinically common reagents, the cost is lower, and the clinical popularization is convenient.
Owner:ZHENGZHOU UNIV +1

Cytochrome P450 enzyme humanized rat model as well as construction method and application thereof

The invention belongs to the technical field of biological medicine, and discloses a construction method of a CYP enzyme humanized rat animal model for drug metabolism research and application of the CYP enzyme humanized rat animal model. The construction method comprises genotype identification, humanized gene expression identification and humanized gene function verification. The method comprises the following steps of firstly, constructing a CYP enzyme humanized rat by utilizing a CRISPR system, including selection of a gene editing target spot, in-vitro synthesis and transcription of sgRNA and Cas9 mRNA, construction of a homologous recombination template, preparation of a pseudopregnant female rat, in-vitro microinjection and transplantation of a single-cell embryo and reproduction of the rat, finally obtaining a homozygote CYP gene humanized rat, then performing CYP enzyme expression detection on the homozygous humanized rat from a protein level, and performing metabolic function verification to prove that the CYP humanized rat is successfully constructed. The CYP1A2 humanized rat has metabolic characteristics more similar to those of people, the species difference of CYP1A2 mediated drug metabolism between the rat and the people is eliminated, and a new rat animal model is provided for research on CYP mediated drug metabolism.
Owner:EAST CHINA NORMAL UNIV

Gene polymorphism detection primer set, kit and detection method of caffeine metabolic capacity related gene CYP1A2

The present invention discloses a gene polymorphism detection primer set, a kit and a detection method of a caffeine metabolic capacity related gene CYP1A2. The gene detection primer set comprises three detection primers and two internal control primers. The present invention provides the primer composition for detecting CYP1A2 gene mutations of samples of fresh blood, etc., and when the primer composition is used for detecting a C5246A mutation of the CYP1A2 gene, the primer composition has advantages of high sensitivity, strong specificity, short time consumption, etc. The kit is simple instructure design and convenient to use. The partition design enables the detection process to be less susceptible to contamination and detection results are more accurate. The detection method is short in time consumption, high in sensitivity and strong in specificity.
Owner:大连美纳医学检验实验室有限公司
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