73results about How to "Good tissue permeability" patented technology

The invention relates to a steroidal derivative as a PD-1 blocker and application thereof, in particular to a compound shown as a formula I below, a medicinal composition containing the compound shownas the formula I below, and application of the compound to treatment of PD-1 mediated related diseases and preparation of medicines for treating the PD-1 mediated related diseases.

The present invention relates to a compound having the formula

where Z is an amine, alcohol, or thiol-containing group, and Y is an alkyl-containing amine. Methods of producing such compounds and using them to treat patients with diabetes and obesity are also disclosed. The present invention also relates to treating such conditions with GADPH inhibitors and screening compounds useful for treating such conditions by using GADPH inhibitors. Compounds can also be screened for their effectiveness in modulating diabetes and obesity with a C. elegans strain.

The invention discloses an anti-human EGFR (epidermal growth factor receptor) nano antibody and an application of the nano antibody. The nano antibody is one or a combination of at least two of an aEG1B4 nano antibody with an amino acid sequence shown as SEQ ID NO: (sequence identifier number) 1, an aEG2C7 nano antibody with an amino acid sequence shown as SEQ ID NO: 2, an aEG2E12 nano antibody with an amino acid sequence shown as SEQ ID NO: 3, an aEG4D9 nano antibody with an amino acid sequence shown as SEQ ID NO: 4 and an aEG6B2 nano antibody with an amino acid sequence shown as SEQ ID NO: 5. The nano antibody has high affinity, specificity and low immunogenicity and the advantages of better stability, simple structure and easy engineering transformation, and can be better applied to development of antibody medicines.

The invention relates to a tetracyclines aptamer, an aptamer electrochemical biological sensor for detection of tetracyclines, and a preparation method and a detection method of the sensor. The tetracyclines aptamer is a single strand DNA probe containing a TTGAGCCCT sequence and having the length of 13-20 bp, and an amino is modified by a 5' end, namely 5'-NH2-(CH2)6-. The aptamer electrochemical biological sensor for the detection of the tetracyclines contains the tetracyclines aptamer. The sensor improves the sensitivity of the detection of the tetracyclines, and can detect the tetracyclines in a minimum concentration of 1.0 ng/mL; and the sensor greatly reduces the cost of the detection of the tetracyclines, has simple and convenient operation, and can rapidly detecting the tetracyclines.

The present invention provides a fusion polypeptide against EB virus-induced tumor, which comprises an antibody or a mimetic antibody against EB virus and an ion channel forming colicin selected form E1, Ia, Ib, A, B, N and their mutants. The present invention also provides a colicin Ia mutant, which comprises mutations of G11A, H22G, A26G, V31L, and H40D. The present invention also provides a gene, vector, preparation method and use of the fusion polypeptide, and provides a gene and use of the mutant.

The invention discloses an individualized beautifying skin care product and a preparation method thereof. The individualized beautifying skin care product is prepared by mixing the following raw materials in percentage by weight: 1 to 20 percent of individualized human-derived immune cell culture supernatant fluid freeze-dried powder expressing hirudin, 1 to 15 percent of grease, 1 to 27 percent of aliphatic ester, 1 to 8 percent of organic solvent, 0.1 to 1 percent of perfume, 5 to 30 percent of nutrient and the balance of ultrapure water. The beautifying skin care product containing individualized immune cell culture supernatant fluid freeze-dried powder expressing the hirudin, disclosed by the invention contains most of purely natural and individualized growth factors which are required by cell growth as well as the hirudin which is transfected by genes and expressed by individualized immune cell secretion, so that immunological rejection can be avoided when the individualized beautifying skin care product is used for beautifying, and the individualized beautifying skin care product has comprehensive effects of dredging skin microcirculation, resisting microthrombus, removing spot and acne, moisturizing skin, whitening, preventing skin ageing and increasing skin elasticity, and is an individualized, efficient and green beautifying skin care product.

A targeting nanoparticle of 10-hydroxy camptothecine for treating tumor is proportionally prepared from gelatin, 10-hydroxy camptothecine, tert-butanol, VC, chitosan, carboxymethyl cellulose sodium, and the water for injection. Its preparing process is also disclosed.

The invention relates to a sodium fusidate powder-injection pharmaceutical composition for injection and a preparation method. Specifically, the invention belongs to the technical field of medicines, relates to a medicine which can be used for treating various infections such as osteomyelitis, sepsis, endocarditis, repeatedly infected cystic fibrosis, pneumonia, skin and soft tissue infections, surgical and traumatic infections and the like caused by various sensitive bacteria, especially staphylococcus, and particularly relates to a pharmaceutical composition such as a freeze-dried powder injection prepared by taking sodium fusidate as an active component. The invention also relates to a preparation method of the pharmaceutical composition. In an implementation scheme, the invention relates to a sodium fusidate powder-injection pharmaceutical composition for injection, which comprises sodium fusidate, a neutral amino acid and an alkaline amino acid. The pharmaceutical composition has excellent pharmaceutical properties.

The invention discloses a cerebral cancer suppressing phycocyanin-polylactic acid-adriamycin micelle. Phycocyanin and PLA-PEG-PLA are utilized as raw materials, and a phycocyanin-polylactic acid no-load micelle is formed according to addition reaction of carboxyl and self-assembly principle based on hydrophilia and hydrophobicity. According to the self-assembly principle, adriamycin is coated in the no-load micelle to assemble by itself to form the micelle. The phycocyanin-polylactic acid-adriamycin micelle is a novel nano medicine capable of directly acting on tumor through blood-brain barrier to suppress cerebral cancer cells and capable of releasing slowly to retain in blood for a long time, thereby overcoming influence and limit of the blood-brain barrier to drug treatment effect. Besides, the micelle is prepared from natural or degradable components which are not involved with organic solvents during synthesis, has the advantages such as good biocompatibility, biodegradability, hypotoxicity, high loading capacity, and accordingly has high application potential in treating cerebral cancer.

Disclosed are ligands that have binding specificity for interleukin-4 (IL-4), for interleukin-13 (IL-13), or for IL-4 and IL-13. Also disclosed are methods of using these ligands. In particular, the use of these ligands for treating allergic asthma is described.

The invention discloses an affinity mature binding protein of an anti-human EGFR and an application. The affinity mature binding protein is an aEG22C4 affinity mature binding protein with an amino acid sequence shown as SEQ ID NO: 4, or a binding protein formed by combining at least one of an aEG12E2 affinity mature binding protein with an amino acid sequence shown as SEQ ID NO: 2, an aEG13E8 affinity mature binding protein with an amino acid sequence shown as SEQ ID NO: 3 and an aEG11A6 affinity mature binding protein with an amino acid sequence shown as SEQ ID NO: 1 with the aEG22C4 affinity mature binding protein. The affinity mature binding protein has the advantages of high affinity, high specificity, low immunogenicity, better stability, simple structure, easiness in engineering transformation and the like, and can be better applied to development of binding protein drugs.

The invention provides a preparation method of a triblock polymer micelle. The preparation method comprises the following steps: (1) enabling chitosan oligosaccharide and dithiodipropionic acid to react under the effect of an activating agent, thus obtaining a first intermediate; (2) enabling the first intermediate and polyethyleneimine to react under the effect of the activating agent, thus obtaining a second intermediate; (3) enabling the second intermediate and urocanic acid to react under the effect of the activating agent, thus obtaining a triblock polymer; and (4) dissolving the triblock polymer obtained in the step (3) in water, thus obtaining the triblock polymer micelle. The triblock polymer micelle has the excellent tissue permeability and enhanced penetration and retention effects, so that a natural passive targeting effect is achieved, and a new candidate system is provided for the development of nanocarriers.

The invention provides a single-domain antibody XHF4RC8 for neutralizing the Xinjiang hemorrhagic fever virus and application thereof in preparing medicine for preventing or treating Xinjiang hemorrhagic fever virus infection. The amino acid sequence of the single-domain antibody XHF4RC8 is shown as SEQ ID NO: 1, and the nucleotide sequence of a gene for coding XHF4RC8 is shown as SEQ ID NO: 2. The VH structural domain m0 of a human antibody IgG1 serves as the framework of the single-domain antibody. XHF4RC8 can be bound with the structural domain III of Xinjiang hemorrhagic fever virus envelope protein Gc and has the virus neutralizing effect. XHF4RC8 is small in molecular weight and has higher tissue penetration and higher capability for being bound with epitope with the steric effect. XHF4RC8 can be expressed in a prokaryotic expression system and is low in production cost and short in production cycle. XHF4RC8 has the potential function of treating the Xinjiang hemorrhagic fever virus clinically or can be used in combination with other antibodies to achieve an ideal treatment effect.

The invention relates to the technical field of protein interaction imaging, and provides a protein fragment complementary system based on split luciferase Akaluc and a construction method thereof. The protein fragment complementary system comprises a first vector and a second vector, the first vector is a vector containing a sequence SEQ ID NO.2, and the second vector is a vector containing a sequence SEQ ID NO.3. The protein fragment complementary system is a complementary system based on the split luciferase Akaluc, the luciferase Akaluc can react with a substrate Akalumine, and fluorescence is generated under the condition of physiological temperature (37 DEG C). Furthermore, the fluorescence generated by the reaction of the luciferase Akaluc and the substrate Akalumine has longer wavelength, so that the fluorescence generated by the protein fragment complementary system has better tissue permeability and is beneficial to imaging observation.

The invention discloses a modified binding protein of EpCAM and application of the modified binding protein. The modified binding protein is at least one of a modified binding protein of which the amino acid sequence is shown as SEQ ID NO.1, a modified binding protein of which the amino acid sequence is shown as SEQ ID NO.2, a modified binding protein of which the amino acid sequence is shown as SEQ ID NO.3 and a modified binding protein of which the amino acid sequence is shown as SEQ ID NO.4. The invention also discloses an application of the binding protein modified by the EpCAM in preparation of antitumor drugs. The binding protein has high structural stability and strong tissue permeability, is human-derived, has no immunogenicity in a human body, and can be better applied to development of antitumor drugs.

A fluorescent probe comprising a compound represented as (Fluorophore A)-S-(Fluorophore B) (Fluorophore A and Fluorophore B are fluorophores which emit fluorescence when they are irradiated with an excitation light of a wavelength of 600 to 950 nm, Fluorophore A has a property that it shows change of fluorescence characteristic before and after a specific reaction with an substance to be measured, and S represents a spacer which connects Fluorophore A and Fluorophore B), which compound shows substantial change in efficiency of fluorescence resonance energy transfer between Fluorophore A and Fluorophore B before and after the specific reaction with the objective substance, wherein Fluorophore A is represented by the following formula (AI):

which uses and shows an excitation light wavelength/fluorescence wavelength in the near infrared region, lights of which region show superior biological tissue permeability, and enables measurement of an substance to be measured by the ratio method.

[Problem]

A problem addressed by the present invention is to provide a novel fluorescent probe having excellent tissue permeability that is capable of detecting the peptidase activity expressed at a high level in cancer cells and the like as a response of long-wavelength red fluorescence.

[Solution]

A compound represented by formula (I) or a salt thereof:

[In the formula, A represents a ring structure selected from the group consisting of a thiophene ring, a cyclopentene ring, a cyclopentadiene ring, and a furan ring;

• X represents a C₀-C₃ alkylene group;
• Y represents O, S, C(═O)O, or NH,
• Z represents O, C(R^a) (R^b), Si(R^a) (R^b), Ge(R^a) (R^b), Sn(R^a) (R^b), Se, P(R^c), or P(R^c) (═O) (where R^a and R^b each independently represent a hydrogen atom or an alkyl group, and R^c represents a hydrogen atom, an alkyl group, or an aryl group);
• R¹ and R² each independently represent from one to three of the same or different substituents selected from the group consisting of a hydrogen atom, a hydroxyl group, a halogen atom, and an alkyl group, a sulfo group, a carboxyl group, an ester group, an amide group, and an azide group each of which may be substituted;
• R³ represents an acyl residue derived from an amino acid (where the acyl residue is a residue obtained by removing an OH group from a carboxyl group of the amino acid);
• R⁴ and R⁵ each independently represent a hydrogen atom or an alkyl group (where when R⁴ or R⁵ is an alkyl group, the R⁴ or R⁵, together with R², may form a ring structure comprising a nitrogen atom to which R⁴ and R⁵ are bonded).]