Pharmaceutical Development and Drug Discovery Research Reagents

Prodrug Ingredients

Prodrug, also known as prodrug, refers to a class of compounds that are inactive or weakly active, which are converted into metabolites or parent drugs with pharmacological activity or significantly enhanced pharmacological activity through enzyme catalysis or non-enzymatic action in the body. Prodrugs can be divided into two categories: Carrier-linked prodrug: The parent drug is linked to the carrier by a covalent bond, and the drug is exerted after the carrier is removed by biodegradation or chemical reaction in the body. The carrier is usually lipophilic and can be a small molecule compound such as a fatty chain, polyethylene glycol, etc., or a large molecule compound such as albumin and antibodies. Bioprecursor prodrug: The active ingredient is chemically modified, and after a series of enzymatic conversions in the body, the parent drug is released to exert its efficacy.

Natural Polymers (for DDS)

Natural polymers refer to high molecular weight compounds extracted from nature, such as polysaccharides, proteins and nucleic acids from plants, animals or microorganisms. Due to their good biocompatibility, biodegradability and diverse functional properties, natural polymers are widely used in the preparation of drug carriers and the development of more efficient and safe drug delivery solutions.

Monomers for Synthetic Polymers (for DDS)

Monomers are small molecules that can be combined together to form polymers through chemical reactions such as polymerization. In DDS, these monomers are usually designed to have specific functions in order to play a specific role in the drug delivery process.

Polyethyleneglycols (PEG) (for DDS)

Polyethylene glycol is a synthetic polymer material widely used in drug delivery systems (DDS). Due to its unique physicochemical properties and good biocompatibility, PEG plays an important role in improving the solubility, stability and bioavailability of drugs.

PEGylation Reagents (for DDS)

PEGylation agents are used to improve the pharmacokinetic properties of drugs or other biomolecules by attaching PEG to them. PEG is a non-toxic, non-immunogenic polymer with high hydrophilicity and flexibility that can increase the solubility of molecules and reduce renal clearance, thereby prolonging the circulation time of drugs in the body. PEGylation agents provide an effective way to improve the pharmacokinetic properties, stability and biocompatibility of drugs in drug delivery systems.

Cyclodextrins (for DDS)

The application of cyclodextrin (CD) in drug delivery systems (DDS) is mainly reflected in its unique structure and function. Cyclodextrin is a type of cyclic oligosaccharide composed of D-pyranose glucose units connected by α-1,4-glycosidic bonds. It usually contains 6, 7, and 8 glucose units, which are called α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin, respectively. Due to its special cylindrical structure, the inner side of the cavity of cyclodextrin is hydrophobic and the outer side is hydrophilic. This structure enables cyclodextrin to encapsulate a variety of organic and inorganic small molecules to form inclusion complexes, thereby changing the properties of these molecules, which can effectively improve the solubility, bioavailability, and targeting of drugs.

Drug Delivery Systems (DDS) Research Reagents (Others)

Phospholipids (for DDS)

Lipids (Other) (for DDS)

Synthetic Polymers (for DDS)

Synthetic polymers have become key materials in the field of modern medicine due to their adjustable physicochemical properties, good biocompatibility and adaptability, and play an important role in drug delivery systems.

Chelating Agents (for DDS)

Chelators play an important role in drug delivery systems. These compounds are able to form stable complexes with metal ions, thereby modulating their bioavailability, improving drug stability, reducing toxicity, or enhancing the therapeutic effect of drugs.

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 and 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 a phosphate group with a sulfur atom. Phosphorothioating agents are particularly useful in the synthesis of thiophosphates and in altering the reactivity of molecules.

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.

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.

Cubane Building Blocks

Cubane, also known as pentacyclic octane, is a synthetic organic compound with a molecular formula of C8H8. Its structural characteristics are that eight carbon atoms are symmetrically arranged at the eight corners of a cube and connected to each other by single bonds. It is a cage-shaped structure and a five-contracted ring system with high tension.

Bicyclo[1.1.1]pentane Building Blocks

Bicyclo[1.1.1]pentane is a bridged ring compound consisting of two rings with a bridgehead carbon atom in the middle. Its molecular formula is C5H8 and it is used in organic synthesis.

Bicyclo[2.1.1]hexane Building Blocks

Bicyclo[2.1.1]hexane is a bridged ring compound consisting of two rings with a bridgehead carbon atom in the middle. Its molecular formula is C6H1 and it is used in organic synthesis.

Bicyclo[3.1.1]heptane Building Blocks

Bicyclo[3.1.1]heptane is a bridged ring compound consisting of two rings with a bridgehead carbon atom in the middle. Its molecular formula is C7H12 and it is used in organic synthesis.

Albumin Binding Fluorescent Probes

Albumin Binding Modification Reagents

Albumin Binding Color Development Reagents

Cross-Linkers

Crosslinkers are mainly used to connect antibodies and toxins. The linker that connects cytotoxic drugs to monoclonal antibodies is the core part of ADC. One of the biggest challenges in developing effective ADCs is to choose a suitable crosslinker. The crosslinker must be able to release the cytotoxic drug in an active form in or near the target cell. The crosslinker is the basis for the effective delivery of cytotoxic drugs by ADC and is also a key factor in determining the toxicity of ADC products. Premature release of drugs in the circulation can lead to systemic toxicity and a lower therapeutic index. The choice of linker usually depends on the target, the drug, the internalization and degradation of the antibody-antigen complex, and the properties of the drug used.

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.

Payload (Drug) Candidates

After ADC drugs enter the blood circulation, they bind to the target antigen receptors on the surface of tumor cells. The newly formed ADC-antigen complex is internalized and degraded by lysosomes, releasing the payload and inducing tumor cell death. The payload is an important component of ADCs, and its activity and physicochemical properties directly affect the anti-tumor efficacy of ADCs drugs. The ideal payload should have sufficiently high cytotoxicity, low immunogenicity, high stability, modifiable functional groups, bystander killing effect, appropriate water solubility, and the target should be intracellular. Common payloads include tubulin inhibitors and DNA damaging agents.