APIs for research and impurities

Palbociclib Impurity F is a high purity synthetic intermediate for the production of Palbociclib. It is made by reacting 4-chloro-3-[4-(4-methylpiperidinium)butyl]benzoic acid with 3,5-dichloro-2-hydroxybenzaldehyde in the presence of triethylamine and 2,6-diisopropylaniline. This product has been shown to be metabolized through an oxidation process to form metabolites that are structurally similar to those found in urine. The chemical structure of this impurity can be found in CAS No. 851067-56-6.

Rac-Benzyl phenylephrone hydrochloride is a synthetic compound that is not found in nature. It can be used as an analytical standard or a pharmacopoeia impurity standard. Rac-Benzyl phenylephrone hydrochloride has been shown to inhibit the activity of CYP3A4, an enzyme which metabolizes many drugs. As a result, it may be useful for drug development and research and could have applications in niche markets such as natural products.

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Cyamemazine sulfoxide is a histamine H1 receptor antagonist. It has been shown to have strong affinity for the serotonin 5-HT2C and dopamine D2 receptors, as well as the atrial 5-HT2A receptors. Cyamemazine sulfoxide has a low oral bioavailability of about 10% and is metabolized in the liver to cyamemazine and its active form, cyamemazine sulfoxide. Cyamemazine sulfoxide binds to serotonin 5-HT2C receptors with a high affinity, which leads to inhibition of serotonin release from nerve endings in the brain. This drug also inhibits dopamine release from nerve endings in the brain and has been shown to have cardiac effects on heart rate and contractility.

Bendamustine isopropyl ester is a synthetic, high purity drug product. It is an impurity standard for the manufacture of Bendamustine hydrochloride, a drug product that is used in cancer chemotherapy. Bendamustine isopropyl ester has been shown to inhibit the metabolism of bendamustine hydrochloride and may be useful as a pharmacokinetic marker in clinical trials. Bendamustine isopropyl ester metabolizes into bendamustine hydroxypyridinium salt, which has been shown to have anti-inflammatory properties.

3'-[3-(3-Azido-2,3-dideoxy-b-D-erythro-pentofuranosyl)-3,6-dihydro-5-methyl-2,6-dioxo-1(2H)-pyrimidinyl]-3'-deoxythymidine is an analytical standard used in the R&D and drug development of 3'-azido derivatives of thymidine. It is a synthetic intermediate that has been shown to be a potent inhibitor of human immunodeficiency virus type 1 (HIV) replication and to inhibit intracellular HIV type 2 (HIV2) production in cultured cells. 3'-[3-(3-Azido-2,3,-dideoxy--b erythro--pentofuranosyl)-3,6--dihydro--5--methyl--2,6--dioxo--1(2H)--pyrimidinyl]-

1-[[3-Methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1H-b enzimidazole is an impurity of a drug product. It is a metabolite that has been shown to be present in human plasma and urine. This compound is synthetically produced and is not found in nature. It has been shown to have niche applications in both analytical chemistry and pharmacopoeia.

Bortezomib impurity 76 is an analytical reference material that is used in the development and production of pharmaceuticals. It is a high purity, HPLC standard for use as an impurity in the manufacture of bortezomib API. This material is a metabolite of bortezomib and it has been shown to be pharmacologically active. Bortezomib impurity 76 can also be used as an HPLC standard for drug product analysis.

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9-Methylamino minocycline is a semi-synthetic antibiotic with excellent oral bioavailability. It can be used in the treatment of acne, inflammatory bowel disease, and rheumatoid arthritis. 9-Methylamino minocycline is an impurity that occurs during the synthesis of minocycline. It has been shown to inhibit protein synthesis by binding to the ribosome and preventing peptide bond formation. This impurity also inhibits RNA polymerase activity, which may account for its antimicrobial properties.

o-Desmethyl venlafaxine N-dimer is a metabolite of venlafaxine that has been identified in human plasma. It is a white to off-white crystalline powder with a melting point of about 175°C. The purity of the product is more than 98%. It is soluble in methanol and ethanol, but insoluble in water. The o-desmethyl venlafaxine N-dimer was developed as an analytical reference standard for use in HPLC analysis of venlafaxine and its metabolites and impurities.

Tetracosanoic acid is a drug product that is used in the development of drugs and as an analytical standard. Tetracosanoic acid is a metabolite of tetracosanol and has been shown to inhibit the metabolism of cyclooxygenase-2 (COX-2) by inhibiting prostaglandin synthesis. Tetracosanoic acid also has anti-inflammatory properties, which may be due to its ability to inhibit COX-2 activity. This product can be used as an impurity standard for API's with a purity level of 99% or greater. Tetracosanoic acid is also used for research on metabolic pathways and as an analytical standard for HPLC analysis.

Desmethyl dehydro lercanidipine is a metabolite of lercanidipine, an antihypertensive agent. Lercanidipine is a dihydropyridine calcium channel blocker that inhibits the influx of calcium ions into cardiac muscle cells and vascular smooth muscle cells. The desmethyl form of lercanidipine has been shown to have anti-inflammatory effects in rats with experimental arthritis. It has also been shown to inhibit the production of inflammatory cytokines in lipopolysaccharide-stimulated human peripheral blood mononuclear cells.

Roxithromycin is a macrolide antibiotic that inhibits protein synthesis in bacteria. It binds to the 50S ribosomal subunit, thereby inhibiting bacterial growth. Roxithromycin has been used to diagnose intestinal and esophageal diseases, inflammatory diseases, and cancer. There are some cardiac effects associated with Roxithromycin that may be related to its ability to inhibit serotonin reuptake. This drug also has anti-inflammatory properties and has been shown to be effective against influenza virus infections as well as other infectious diseases such as tuberculosis and HIV/AIDS.

6-O-Desmethyl moxonidine is a drug product that is a metabolite of the parent compound, moxonidine. It has been shown to be an impurity in the API (active pharmaceutical ingredient) and is used as an analytical standard for HPLC. 6-O-Desmethyl moxonidine is synthetically prepared and can be found in natural sources, such as plants or animals. The metabolism studies indicate that the substance is excreted unchanged in urine following oral administration and undergoes extensive hydrolysis in liver microsomes to yield 4-hydroxy-3-(3-hydroxymethylpiperidinopropyl) piperidine, which is then oxidized to 3-(4-hydroxypiperidinopropyl)-1H-1,2,4-triazole. This product may cause skin irritation.

Ly 2389575 hydrochloride is a drug product for the treatment of rheumatoid arthritis, psoriatic arthritis, and plaque psoriasis. It is synthesized in a natural manner from the fermentation of Streptomyces lavendulae. The compound has been shown to be metabolized through a number of metabolic transformations including hydrolysis by esterases or glucuronidases, oxidation by cytochrome P450 enzymes, reduction by glutathione reductase, or conjugation with glucuronic acid. Ly 2389575 hydrochloride also specifically binds to markers expressed at high levels in Mycobacterium tuberculosis strains (e.g., ESX-1 secretion system protein) and inhibits cell growth in culture.

2,2'-(1,4-Piperazinediyl)bis[6,7-dimethoxy-4-quinazolinamine] is a chemical compound that is used as a lead to develop new drugs against malaria. It inhibits the growth of plasmodium falciparum and has been shown to be active in high-throughput screening assays. 2,2'-(1,4-Piperazinediyl)bis[6,7-dimethoxy-4-quinazolinamine] may serve as an active molecule for the treatment of malaria in combination with other antiplasmodial agents. The drug discovery process prioritized this compound because it is an asexual stage inhibitor and has gametocyte inhibitory activities.

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Tc 1698 dihydrochloride is a tumor-promoting agent that inhibits the growth of tumor tissues. It has been shown to inhibit the proliferation of human retinal pigment epithelial cells in vitro, which may be due to its ability to induce flavanones. Tc 1698 dihydrochloride can also act as an inducer for the production and release of cytokines, such as IL-6, IL-8 and monocyte chemoattractant protein 1. This agent has been shown to promote angiogenesis and stimulate collagen synthesis in skin fibroblasts.