Nucléosides et Nucléotides

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (

Dinotefuran (MTI-446), a neonicotinoid insecticide, targets pests by blocking their nervous system.

Applications A metabolite of (-)-Emtricitabine (E525000). References Schinazi, R.F., et al.: Antimicrob. Ag. Chemother., 36, 2423 (1992); Shockeor, J.P., et al.: Xenobioica, 26, 189 (1996); Feng, J.Y., et al.: FASEB J., 13, 1511 (1999); Molina, J.-M., et al.: J. Infec. Dis., 182, 599 (2000);

Vitamin B6 aids metabolism, especially for amino acids, and helps prevent pregnancy-induced and radiation sickness vomiting.

AKR1C3-IN-4: potent, selective AKR1C3 inhibitor, IC50 = 0.56 μM, potential for CRPC research.

Triphenylmethanol (TPM) is an inhibitor of the enzyme alcohol dehydrogenase. It is synthesized by reacting p-hydroxybenzoic acid with a hydroxyl group in the presence of trifluoroacetic acid and potassium carbonate. The reaction solution was then analyzed by x-ray crystallography, revealing the molecular structure of TPM. TPM binds to the metal ion in a hydroxyl group, preventing alcohol dehydrogenase from oxidizing ethanol to acetaldehyde. This mechanism also explains why TPM inhibits other enzymes that use this same metal ion cofactor such as carboxypeptidase A and aminopeptidase P, which are involved in protein synthesis and degradation. Triphenylmethanol (TPM) is an inhibitor of the enzyme alcohol dehydrogenase. It is synthesized by reacting p-hydroxybenzoic acid with a hydroxyl group in the presence of trif

2-Deoxy-5-O-toluoyl-D-ribofuranose is an analytical standard for the determination of purity in drug products. It is also used as a reference compound for HPLC and as a metabolite to study metabolism. This impurity can be synthesized from D-ribose and 2(3,4,5)-O-benzylidenebutyraldehyde.

Cangrelor tetrasodium is a reversible and selective antagonist of platelet P2Y12, with prompt and potent antiplatelet effects.

Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor.

Applications Widespread throughout animal and plant tissues combined with niacinamide, d-ribose, and phosphoric acids; a constituent of nucleic acids and coenzymes, such as codehydrase I and II, adenylic acid, coalaninedehydrase. It is used in microbial determination of niacin; in research on heredity, virus diseases, and cancer. References Philips, et al.: J. Pharmacol. Exp. Ther., 20, 104 (1952), Lambertucci, C., et al.: Bioorg. Med. Chem., 17, 2812 (2009),

2-Acetamido-9-[2-(acetyloxy)ethoxy]methyl-6,9-dihydro-1H-purin-6-one (ademetionine) is a prodrug that is metabolized in the liver to form ademetionine. Ademetionine is a potent inhibitor of guanosine deaminase, which is an enzyme that breaks down guanosine into guanine and ammonia. Ademetionine has shown efficacy in cancer treatment and may also be used to treat tuberculosis. The metabolism of this drug takes place in the liver, where it undergoes oxidation by cytochrome P450 enzymes to form the active metabolite ademetionine. Metabolism of this drug can be inhibited by drugs such as trifluoromethanesulfonic acid (TFMS), which are used for the treatment of malaria. TFMS inhibits the formation of ademetionine but does not affect the formation

Stability Hygroscopic Applications A potent adenosine receptor agonist. Inhibits platelet aggregation and is centrally active in vivo. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Cusack and Hourani: Br. J. Pharmacol., 72, 433 (1981), Knapp, et al.: Pharmacol. Biochem. Behav., 68, 797 (2001)

Applications Favipiravir is used for the treatment of advanced Ebola virus infection in a small animal model. Favipiravir suppressed the replication of Zaire Ebola virus and prevented a lethal outcome in 100% of the animals. Based on the studies, Favipiravir can be a candidate for the treatment of Ebola hemorrhagic fever. It is a COVID19-related research product. References Oestereich, L., et al.: Antiviral Res., 105, 17 (2014); Baranovich, T., et al.: J. Virol. 87, 3741 (2013); Chem. and Eng. News p.8, Dec. 1 (2014)

Meropenem EP impurity A is a heterocyclic nitro compound that is used to treat various infectious diseases. Meropenem EP impurity A is an inhibitor of the toll-like receptor, which is a protein that recognizes and binds to bacterial lipopolysaccharide and mediates inflammation. This drug may be effective in treating colorectal carcinoma, autoimmune diseases, chronic bronchitis, cancer, and other inflammatory diseases. Meropenem EP impurity A also has anti-cancer properties due to its structural similarity with the chemotherapeutic agent 5-fluorouracil. Meropenem EP impurity A inhibits the synthesis of proteins by binding to the aminoacyl-tRNA synthetase enzyme and blocking the production of proteins vital for cell division.

1,5-Isoquinolinediol, a PARP1 inhibitor (IC50: 0.39 μM), is used in DNA repair and cell death studies.