Pharmaceutical Development and Drug Discovery Research

Aldehyde Reactive Fluorophores and Labels

Aldehyde-reactive fluorescent dyes form stable complexes by covalently binding to amino, hydroxyl and other functional groups in biomolecules. This reaction usually involves the formation of imine or ether bonds to achieve labeling. These fluorescent markers have a wide range of applications in biomedical research, cell imaging, protein labeling and other chemical analysis.

Amino Acid Azides/Alkynes

Amino acid azides are a class of compounds that introduce an azide group (-N₃) into amino acid molecules. Amino acid alkynes are amino acids containing an alkyne group. The alkyne-azide group is a highly active functional group that can participate in

Trialkoxysilane Azides/Alkynes

Trialkoxysilane azides are trialkoxysilanes containing an azide, and trialkoxysilane alkynes are trialkoxysilanes containing an alkyne group. The alkyne-azide group is a highly reactive functional group that can participate in a variety of chemical reactions, especially click chemistry reactions such as the CuAAC (copper-catalyzed azide-alkyne cycloaddition) reaction.

Carbohydrate Azides/Alkynes

Carbohydrate azides/alkynes are carbohydrates containing an azide, and carbohydrate alkynes are carbohydrates containing an alkyne group. The alkyne-azide group is a highly reactive functional group that can participate in a variety of chemical reactions, especially click chemistry reactions such as the CuAAC (copper-catalyzed azide-alkyne cycloaddition) reaction.

Catalysts, Ligands, Reagents

Copper-free Click Reaction Reagents

Copper-free click chemistry is a chemical reaction method that can achieve rapid intermolecular connection under mild conditions without the use of toxic copper catalysts. Copper-free click reaction reagents mainly include DBCO (dibenzocyclooctyne) and BCN (benzocyclooctyne) compounds. These reagents can react with azides under copper-free conditions to form stable triazole bonds. They are often used in biomedicine, materials science, and drug development.

Fluorophore Azides/Alkynes

A fluorinated azide or alkyne-containing group, alkyne, is a highly reactive functional group that can participate in a variety of chemical reactions, especially click chemistry reactions such as CuAAC (copper-catalyzed azide-alkyne cycloaddition) reactions.

Biotin Azides/Alkynes

Biotin azide or alkyne-containing groups, alkyne, azide group is a highly reactive functional group that can participate in a variety of chemical reactions, especially click chemistry reactions such as CuAAC (copper-catalyzed azide-alkyne cycloaddition) reaction.

Nucleoside Azides/Alkynes

Nucleoside azide or alkyne-containing groups, alkynes, azide groups are highly reactive functional groups that can participate in a variety of chemical reactions, especially click chemistry reactions, such as CuAAC (copper-catalyzed azide-alkyne cycloaddition) reactions. Widely used in biological and cytological research

Crosslinker Azides/Alkynes

Cross-linker azides are a class of compounds containing an azide group (N3), and cross-linker alkynes are a class of compounds with an alkynyl (-C≡C-) functional group, which are widely used in drug delivery, biomarkers and other fields.

PEG Azides/Alkynes

Polyethylene glycol azide/alkyne is a class of polyethylene glycol (PEG) derivatives with azide groups/alkynes. Polyethylene glycol is a commonly used biocompatible polymer, widely used in drug delivery, medical devices, and biomarkers. Introducing azide groups/alkynes into PEG can significantly enhance its application potential in "click chemistry"

Terminal Alkynes

In the "click chemistry" reaction, terminal alkynes are often combined with azides to form 1,2,3-triazole compounds through the "azide-alkyne" reaction. This process is simple, efficient and highly selective.

Tetrazines

Tetrazine is a six-membered heterocyclic compound containing four nitrogen atoms. It has high reactivity, especially in the click reaction with alkynes, which shows rapid, highly selective and stable characteristics. 12 This reactivity of tetrazine makes it widely used in the fields of biomolecule labeling, drug delivery and bioimaging.

Azides

Azide click chemistry is a chemical process that forms a stable triazole bond by reacting azides with alkynes under mild conditions. This reaction is widely used in biomolecule labeling, drug delivery and bioimaging due to its mild conditions, fast reaction speed and good biocompatibility.

trans-Cyclooctenes (TCO)

Trans-cyclooctene (TCO) is an eight-membered ring structure with a double bond, in which the double bond is in trans (E-type) configuration. This structure enables the TCO portion to undergo efficient bioorthogonal reactions with specific compounds (s

Enzyme Cleavable Linkers (Cleave Motif)

There are specific enzymes in the intracellular lysosomes and tumor microenvironment that can selectively cleave linkers. For example, cathepsins in lysosomes can hydrolyze peptide bonds, such as dipeptide or tetrapeptide linkers. Glycosidases that hydrolyze β-glucuronide and β-galactosidase, phosphatases that hydrolyze pyrophosphate and pyrophosphate, and sulfatases that hydrolyze sulfates.

Biotins, Streptavidins

Biotin was once known as coenzyme R and vitamin H. Biotin is water-soluble, which means that the body does not store it. It has many important functions in the body. It is required for the function of a variety of enzymes, called carboxylases. These biotin-containing enzymes are involved in important metabolic pathways, such as the production of glucose and fatty acids. Streptavidin is a 52.8 kDa protein purified from Streptomyces avedini. Streptavidin homotetramers have an extremely high affinity for biotin. The binding of biotin to streptavidin is one of the strongest non-covalent interactions known in nature, with a dissociation constant of approximately 1 μmol/L. Streptavidin is widely used in molecular biology and bionanotechnology due to the resistance of the streptavidin-biotin complex to organic solvents, denaturants, detergents, proteolytic enzymes, and extremes of temperature and pH.

Functionality Creating Reagents

In bioconjugation, functional groups are used to link two or more molecules via covalent bonds. Functional reagents are used to introduce new reactive groups to target molecules or linkers. Despite the diversity of various molecules, four major chemical targets on target molecules account for most bioconjugation techniques: Primary amines (-NH2): can be crosslinked using NHS (N-hydroxysuccinimide) esters and water-soluble Sulfo-NHS esters. Carboxyl groups (-COOH): can be crosslinked to amino groups via peptide bonds. Thiol/sulfhydryl groups (-SH): can be linked together via disulfide bonds (-SS-). Aldehyde groups (-CHO): are usually generated in molecules by oxidation of carbohydrate groups, including glycoproteins, and can be crosslinked to molecules containing amino or hydrazine groups.

Functional Group Blocking Reagents

Functional group blockers are a class of substances that can bind to receptors and prevent agonists from producing effects. They occupy the active site or allosteric site of the receptor, preventing the binding of agonists to receptors, thereby inhibiting the activity of receptors. Blockers have affinity for the corresponding receptors, but have no efficacy, so they can inhibit the effect of agonists on receptors.

Heterobifunctional Cross-Linkers

Heterobifunctional crosslinkers have different reactive groups at both ends. These crosslinkers can not only couple molecules with their respective target functional groups in a single step, but also in a sequential (two-step) manner, minimizing unwanted aggregation or self-coupling. They are often used in biochemical and biomedical research, especially in protein modification, protein coupling, and protein interaction studies.

PEGylation Reagents and PEG Spacers

Pegylation reagent is an advanced pharmaceutical molecule modification technology that couples polyethylene glycol (PEG) to the surface of drug molecules to change the solubility of the drug, reduce enzymatic hydrolysis, reduce immunogenicity, prolong the half-life, and change tissue distribution, thereby increasing the concentration of the drug in the target area and achieving long-acting drug.

Zero-length Crosslinkers

Zero-length crosslinkers are special chemicals that can form crosslinks between two or more polymer chains without the use of any external additives, thereby improving the physical and chemical properties of the polymer. The chemical structure of zero-length crosslinkers usually consists of two parts: one part is a highly reactive functional group, such as a bifunctional group or a dead group, and the other part is an inactive group, such as an alkyl group, an aryl group, etc. These inactive groups can form stable chemical bonds between polymer chains, thereby achieving the purpose of crosslinking.

Albumin Binding Modification Reagents

Homobifunctional Cross-Linkers

Homobifunctional crosslinkers contain two or more identical reactive groups in their structure. These reactive groups can react with the molecules to be crosslinked to form a crosslinked structure. Since the reactive groups of these crosslinkers are the same, they can react with the same type of reactive groups.

Copper-free Click Reaction Reagents

Copper-free click chemistry is a chemical reaction method that can achieve rapid intermolecular connection under mild conditions without the use of toxic copper catalysts. Copper-free click reaction reagents mainly include DBCO (dibenzocyclooctyne) and BCN (benzocyclooctyne) compounds. These reagents can react with azides under copper-free conditions to form stable triazole bonds. They are often used in biomedicine, materials science, and drug development.

Photo-reactive Crosslinkers

Photoreactive crosslinkers are a class of compounds that can initiate chemical crosslinking reactions by light irradiation. Aryl azides (AZs), benzophenones (BPs), diaziridines (DAs) and 2-aryl-5-carboxytetrazoles (ACTs). Under ultraviolet excitation of a specific wavelength, the corresponding intermediates are nitrene, diradical, carbene and carboxynitrile imine. Among them, carbene-mediated photoaffinity labeling is widely used in drug target recognition.

N-Terminal Cysteine Residue-specific Conjugation Reagents

N-Terminal Cysteine Residue-specific Conjugation Reagents are a class of highly selective chemical reagents that react specifically with the N-terminal cysteine residue (Cys) of proteins or peptides. These reagents have important applications in biochemistry and drug development, especially in labeling, purification, and drug delivery.

Methylated Nucleosides

Methylated nucleoside monomers have many functions in biological and medical research. They not only affect gene expression and nucleic acid stability, but also play an important role in drug development and disease diagnosis. These characteristics make them an important target of modern biology. An important tool in technology and drug research.

Protecting Agents for Hydroxy and Amino Groups

Protective nucleoside monomers refer to protective groups used to avoid unnecessary side reactions in chemical reactions when synthesizing nucleosides or nucleic acids. These protective groups play a key role in protecting nucleosides during the synthesis process.

Phosphorylating Agents, Phosphorothioating Agents

Phosphorylating agents are chemicals that can introduce a phosphate group into a molecule. Phosphorylation is a key process in biochemistry that is involved in regulating protein function, cell signaling, and various biochemical pathways. Phosphorothioating agents are chemicals that can introduce a thiophosphate group into a molecule. Phosphorothioation is a modification that replaces the oxygen atom in the phosphate group with a sulfur atom.

Coupling Activators, Condensing Agents

Coupling activators promote the activation of functional groups (such as carboxyl or amine groups), making them more reactive and promoting the formation of chemical bonds, such as amide bonds or ester bonds. Condensing agents promote the removal of water or other small molecules in the condensation reaction, pushing the equilibrium toward the desired product and improving the reaction yield.

Riboses, 2'-Deoxyriboses

Ribose is a component of RNA and is involved in energy metabolism and cell signaling. 2'-deoxyribose is a component of DNA and ensures the stability of DNA and the long-term preservation of genetic information. The main difference between 2'-deoxyribose and ribose is the hydroxyl group on the 2' carbon, which makes DNA more stable than RNA.

Sulfur Transfer Reagents

Sulfur transfer reagents are widely used in organic synthesis, biochemical research, and materials science by facilitating the transfer of sulfur atoms. These reagents help generate or modify sulfur-containing compounds and play an important role in catalysis, molecular labeling, and structural modification.

Protected Nucleosides

Protected nucleosides are mainly used in the synthesis of nucleic acids and their derivatives in chemical and biological research. The role of protecting groups is to prevent the active groups of nucleosides (such as hydroxyl, amino, etc.) from undergoing undesirable reactions in chemical reactions, thereby improving the selectivity and yield of the synthesis. They are often used in nucleic acid synthesis, such as the synthesis of DNA or RNA, to ensure that specific reaction steps do not damage the structure of the synthesized part.

Nucleoside Phosphoramidites

Phosphoramidite monomers are widely used in the chemical and pharmaceutical fields. In the chemical field, phosphoramidite monomers are mainly used to prepare polymer materials such as polyamide and polyimide. In the pharmaceutical field, especially in the fields of molecular biology and genetics, phosphoramidite monomers also play an important role. For example, in the synthesis of DNA and RNA, phosphoramidite monomers are an important raw material. They can react with amine groups to form phosphoramide bonds, connect deoxyribose or ribose to bases, and thus construct DNA and RNA molecules. Secondly, phosphoramidite monomers can also be used in gene therapy, such as synthetic gene vectors (plasmids and viral vectors).

Peptide Nucleic Acid (PNA) Monomers

Peptide nucleic acid (PNA) is a new nucleic acid sequence-specific reagent. Unlike traditional nucleic acids such as DNA and RNA, it replaces the sugar-phosphate main chain with a polypeptide backbone. Its main features and functions are as follows: 1. Unique structure: PNA molecules are composed of multiple amino acid residues connected by hydrogen bonds. Its structure is different from DNA and RNA, and it has a unique double helix structure and spatial configuration. 2. Highly selective recognition: PNA molecules can bind to specific DNA or RNA sequences to form stable complexes. Due to its unique structure, PNA has a higher binding ability to DNA and RNA than traditional nucleic acid probes. 3. Non-radioactive labeling: Compared with traditional radioactive labeling methods, PNA can be labeled by non-radioactive methods such as chemical synthesis, avoiding the potential harm of radiation to the human body. 4. Good stability: PNA molecules are stable in aqueous solution, do not undergo photolysis, hydrolysis and other reactions, and can be stored and used for a long time.

Base Modified Nucleosides and Nucleotides

Base-modified nucleosides and nucleotides play important roles in gene regulation, cell signaling, molecular recognition, and disease mechanisms, and are crucial for the maintenance and regulation of life processes.

2'-O-Methylribonucleosides

In biomedical research and drug development, 2'-O-methyl ribonucleosides are important modifications that can be used to design more stable RNA molecules to improve their effectiveness as therapeutic drugs.

Amine Protection

In peptide synthesis, especially in solid-phase synthesis and liquid-phase synthesis, the amino group of the amino acid needs to react with the carboxyl group to form a peptide bond. The amino protecting group can protect the amino group from interference from other reactants, thereby achieving selective synthesis of the target sequence.

Amino Acid Derivatives

Amino acid derivatives refer to new compounds obtained by chemically modifying the side chains, amino groups or carboxyl groups of natural amino acids. Common modifications include substitution reactions, acylation, phosphorylation, methylation, etc.

Peptide Coupling Agents

Peptide coupling agents are chemical reagents used to promote the connection between amino acids or polypeptides. In the process of peptide synthesis, peptide coupling agents can effectively react the carboxyl group of an amino acid with the amino group of another amino acid to form a peptide bond. By using these coupling agents, the efficiency and selectivity of the reaction can be improved and the generation of by-products can be reduced. They are used in the synthesis of targeted drugs to enhance the stability and biological activity of drugs.

Precursors for Amino Acid Synthesis

Amino acid synthesis precursors refer to starting materials or intermediates used to generate amino acids during biosynthesis or chemical synthesis. These precursors can be simple small molecules or other types of amino acids, amides or related compounds.

Amino Acid Sequencing Reagents

Amino acid sequencing reagents are chemical reagents used to determine the sequence of amino acids in proteins or peptides. These reagents play a vital role in analyzing the structure, function and biological activity of biomolecules. They mainly include Edman degradation reagents and dansyl chloride.

Solvents and Mixtures for Peptide Synthesis

Commonly used solvents and mixtures in peptide synthesis include DMF (N,N-dimethylformamide), DMSO (dimethyl sulfoxide), DMAc (N,N-dimethylacetamide) and TFE (trifluoroethanol).

Unnatural Amino Acid Derivatives

Non-natural amino acid derivatives refer to amino acids that do not exist in nature or are present in very small amounts. They are usually obtained by artificial synthesis or chemical modification of natural amino acids. These derivatives have diverse side chain groups and unique chemical properties and can be introduced into engineered proteins through genetic codon expansion, metabolic labeling, or protein full/semi-synthesis technology. They are widely used in biochemistry, drug development, materials science and other fields.

mPEG (Methyl Polyethylene Glycols)

mPEG refers to a polymer formed by introducing methyl (-CH₃) side groups through chemical modification based on polyethylene glycol. mPEG has good water solubility, wettability, lubricity and physiological inertness, and is mild and non-irritating to the

Monofunctional PEG and Oligoethylene Glycols

Monofunctional polyethylene glycol (PEG) contains a single chemically reactive end and is commonly used for PEGylation, surface grafting, and nanoparticle coating. Monofunctional PEG is commonly used in bioconjugation, surface functionalization, and nanoparticle coating. Oligopolyethylene glycol (such as PEG-2, PEG-4) is mainly used as a solvent and penetration enhancer to promote the dissolution of active ingredients, improve stability and solubility, enhance the permeability and absorption of oral drugs, and thus improve bioavailability.

Heterobifunctional PEG and Oligoethylene Glycols

Heterobifunctional polyethylene glycol (PEG) has different functional groups at each end of the PEG chain. These linkers allow selective conjugation between two different molecules or surfaces. It is widely used in bioconjugation reactions to connect different molecules or surfaces to achieve specific chemical and biological functions. Oligopolyethylene glycol (such as PEG-2, PEG-4) is mainly used as a solvent and penetration enhancer to promote the dissolution of active ingredients, improve stability and solubility, enhance the permeability and absorption of oral drugs, and thus improve bioavailability.

PEG Oligomers

Polyethylene glycol oligomers are low molecular weight polymers formed by polymerization of ethylene glycol molecules. They have short molecular chains and relatively low molecular weight, so they have some special physical and chemical properties. Polyethylene glycol oligomers have good solubility and permeability, can form stable solutions in water, and easily interact with other substances. They are widely used in biomedicine, cosmetics, and food industries.

PEG Polymers

Polyethylene glycol (PEG), also known as polyethylene oxide (PEO) or polyoxyethylene (POE), refers to oligomers or polymers of ethylene oxide. Polyethylene glycol has excellent lubricity, moisturizing and dispersibility, and can be used as a softener and antistatic agent. It is widely used in cosmetics, pharmaceuticals, chemical fibers, rubber, plastics, papermaking, paints, electroplating, pesticides, metal processing and food processing industries.

Homobifunctional PEG and Oligoethylene Glycols

Homobifunctional polyethylene glycol refers to a PEG molecule with two identical reactive groups. This structure enables it to form crosslinks or connections with other molecules or materials, and is often used to construct multifunctional nanocarriers or crosslinked polymers. Oligopolyethylene glycol (such as PEG-2 and PEG-4) is mainly used as a solvent and permeation enhancer to promote the dissolution of active ingredients, improve stability and solubility, enhance the permeability and absorption of oral drugs, and thus improve bioavailability.

Heterobifunctional Cross-Linkers

Heterobifunctional crosslinkers have different reactive groups at both ends. These crosslinkers can not only couple molecules with their respective target functional groups in a single step, but also in a sequential (two-step) manner, minimizing unwanted aggregation or self-coupling. They are often used in biochemical and biomedical research, especially in protein modification, protein coupling, and protein interaction studies.

Homobifunctional Cross-Linkers

Homobifunctional crosslinkers contain two or more identical reactive groups in their structure. These reactive groups can react with the molecules to be crosslinked to form a crosslinked structure. Since the reactive groups of these crosslinkers are the same, they can react with the same type of reactive groups.

Staudinger Ligation

Staudinger Ligation refers to the process of using phosphine to react with an active carbonyl group (such as amide or ester) to form an intermediate, and then subsequent chemical transformation to generate a stable connection product. It provides an efficient and specific method for labeling, cross-linking and modification of biomolecules.

Photo-reactive Crosslinkers

Photoreactive crosslinkers are a class of compounds that can initiate chemical crosslinking reactions by light irradiation. Aryl azides (AZs), benzophenones (BPs), diaziridines (DAs) and 2-aryl-5-carboxytetrazoles (ACTs). Under ultraviolet excitation of a specific wavelength, the corresponding intermediates are nitrene, diradical, carbene and carboxynitrile imine. Among them, carbene-mediated photoaffinity labeling is widely used in drug target recognition.