Quinazoline and Quinoline Derivatives

Regorafenib metabolite M2 oxide (M2O) is a cancer drug that is an inhibitor of multikinase. It was developed as a prodrug for regorafenib, which is used to treat patients with metastatic colorectal cancer and has been shown to be effective against other cancers, such as lung and pancreatic cancer. M2O inhibits the efflux of drugs from cells by binding to the transporter protein P-glycoprotein. This prevents the accumulation of toxic concentrations of regorafenib in cells, which are responsible for its side effects, such as diarrhea and liver damage. The uptake of M2O by cells is also inhibited by light and acidic conditions. Oral administration of M2O leads to increased exposure to regorafenib in the body because it is not metabolized by CYP3A4 enzymes.

Salbutamol Impurity D is a chiral, metal chelator impurity of the drug substance Salbutamol. It is a prodrug that is hydrolyzed to its active form, salbutamol sulfate, in vivo. Salbutamol Impurity D binds to chloride ions and has been shown to be an interferent for many analytical methods. The reversed-phase chromatography retention time for Salbutamol Impurity D is about 10 minutes shorter than for Salbutamol sulfate.

Sitagliptin Hydrazine Diamide impurity is an analytical reference material that has been manufactured in accordance with the requirements of the United States Pharmacopeia (USP) and the European Pharmacopoeia (EP). The material is a white to off-white crystalline powder. It has a purity of 99.9% with a specific gravity of 1.06 g/cm3 and a melting point of 176-177°C. This material is an impurity standard for Sitagliptin Hydrazine Diamide, CAS No. 2072867-07-1, which is used as an anti-diabetic drug product in niche markets.

5-O-Desethyl amlodipine is a metabolite of amlodipine. It has been used as an analytical reference standard for the determination of amlodipine and its metabolites in human plasma and urine. 5-O-Desethyl amlodipine has been reported to be excreted in human breast milk at a concentration that is about 20% of that found in maternal plasma. The drug product is manufactured by HPLC and is classified as a high purity pharmaceutical drug, which means it is free from extraneous substances such as other drugs, proteins, or bacteria.

Cis-Tadalafil is a potent inhibitor of phosphodiesterase 5, which is used to treat erectile dysfunction (ED) and primary pulmonary hypertension (PPH). It works by increasing blood flow to the penis, allowing men with ED to achieve and maintain an erection. Cis-Tadalafil is also used to treat symptoms of prostatic hyperplasia (enlarged prostate) in men. This drug has been shown to be effective in treating PPH by reducing pulmonary arterial pressure and improving exercise capacity. Cis-Tadalafil belongs to the carboline class of drugs and is a phosphodiesterase 5 inhibitor that selectively inhibits cGMP-specific phosphodiesterase type 5 (PDE5). This drug has been shown to be highly effective in treating both ED and PPH with minimal side effects.

Roflumilast impurity A is a metabolite of roflumilast. It is a drug product that is used as an analytical standard for the determination of roflumilast in HPLC analysis. Roflumilast impurity A is not natural and is synthetic. It has been shown to be a substrate for CYP1A2, CYP2C8, CYP2C9, and CYP3A4 enzymes. Studies have shown that it may be involved in the metabolism of roflumilast through hydroxylation and deamination.

Linagliptin impurity G is an impurity in the drug product Linagliptin. It is a natural substance and its CAS number is 668270-11-9. Impurity G can be synthesized from L-phenylalanine and cyclohexane carboxaldehyde in a two step process. The first step involves the reaction of L-phenylalanine with cyclohexane carboxaldehyde to yield methylcyclohexanecarboxylate, which then undergoes hydrolysis to give phenylcyclohexanol. In the second step, phenylcyclohexanol reacts with hydrochloric acid to produce phenylcyclohexanone, which is then oxidized with hydrogen peroxide to yield impurity G. Impurity G can also be found in the pharmacopoeia as a high purity HPLC standard for linagliptin.

(S)-Rabeprazole sodium is an anticancer drug that acts as a kinase inhibitor. It is an analog of Rabeprazole and has been shown to inhibit the growth of cancer cells in vitro and in vivo. (S)-Rabeprazole sodium inhibits the activity of kinases, which are enzymes that play a key role in cell signaling pathways. This inhibition leads to apoptosis, or programmed cell death, in cancer cells. (S)-Rabeprazole sodium has been tested against various types of cancer, including Chinese hamster ovary cells and tumor xenografts in mice. It has also been shown to inhibit elastin degradation, which is important for preventing metastasis of cancer cells. (S)-Rabeprazole sodium may be a promising candidate for the development of new anticancer drugs that target specific kinases and proteins involved in cancer cell growth and survival.

Empagliflozin S-furanose is a Custom synthesis drug product. It is an analytical standard with CAS No. 1620758-32-8, and it is used in research and development of new drugs. Empagliflozin S-furanose has been found to be a metabolite of empagliflozin, a drug that is used to treat type 2 diabetes mellitus. It is also used as an impurity standard for HPLC analysis of empagliflozin because it does not have any biological activity.

Pramipexole EP Impurity C is a synthetic impurity that is used as an impurity standard in the manufacture of Pramipexole EP. It is also used as a research and development tool for drug product, custom synthesis, CAS No. 1973461-14-1, and analytical studies. This compound has been shown to be a metabolite of Pramipexole EP and may have pharmacological properties. Pramipexole EP Impurity C has been found to inhibit the growth of certain bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA) isolates.

Desfluoro ezetimibe is a synthetic cholesterol-lowering drug that inhibits intestinal cholesterol absorption. It is chemically synthesized, and the process includes the introduction of fluorine at the 3-position of the C-ring. Desfluoro ezetimibe is not metabolized in humans, but it may be subject to oxidative degradation. The product is also subject to oxidation by light and air, which may result in formation of impurities. The drug substance has been validated as well as its isomers and efficiencies in mass spectrometry detection.