Étalons pharmaceutiques

Tibolone is a synthetic steroidal estrogen with both estrogenic and progestogenic activity. It has been shown to be effective in the treatment of postmenopausal symptoms, especially those related to the breast. Tibolone is also used for prevention of osteoporosis and to prevent recurrence of hormone-dependent cancers such as breast cancer or endometrial cancer. Tibolone binds to both estrogen receptor subtypes (ERα and ERβ) and progesterone receptor (PR), but with higher affinity for ERβ. This leads to increased levels of circulating estradiol and progesterone when compared to other estrogens such as nomegestrol acetate or conjugated equine estrogen. The drug also decreases expression of genes that are regulated by the response element (RE) in ERβ-positive cells, which may contribute to its anti-cancer effects. Tibolone has been shown to be statistically more effective than nomegestrol acetate in reducing hot flashes

Androsterone sulfate sodium is a fine chemical that is used as a versatile building block in the synthesis of complex compounds. It is also a valuable reagent in research and speciality chemicals. Androsterone sulfate sodium is used as a high-quality reaction component and can be used as an intermediate to produce other useful compounds. This compound has the CAS number 1852-41-1 and can be used as a scaffold to generate other related compounds.

Cresyl violet acetate is a dye that is used in histology to stain tissue sections. It binds to basic proteins, such as those found in the cytoplasm and nucleus, and has a strong affinity for nucleic acids. Cresyl violet acetate can be used to identify inflammatory lesions and other biological samples. The dye has been shown to induce neuronal death by reducing the redox potentials of neurons through the activation of Toll-like receptors (TLRs). Basic proteins are also involved in oral hypoglycaemic activity.

Applications An intermediate for the synthesis of a benzimidazole PARP inhibitor I (succinate salt) (ABT-472).
References Denny, W., et al.: J. Med. Chem., 33, 814 (1990), Anon., et al.: Curr. Med. Chem., 10, 321 (2003),

Applications Protected Paclitaxel.

Applications DL-10-Camphorsulfonyl Chloride is used as a the starting material in the synthesis of 10-Camphorsulfonic Acid Ethyl Ester (C175040). It is also used as a reagent in the synthesis of 1-benzhydrylpiperazine derivatives which can exhibit antiproliferative activity in vitro against human cancer cell lines.
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 Ananda Kumar, C.S., et al.: Eur. J. Med. Chem., 44, 1223 (2009)

Applications α-(Dibutylamino)-4-methoxy-benzeneacetic Acid is an intermediate in the synthesis of Ambucetamide (A575935). Ambucetamide is an antispasmodic found to be particularly effective for the relief of menstrual pain.
References Janssen, P., et al.: J. Am. Chem. Soc., 76, 6192 (1954); Pickles, V., et al.: 15, 128 (1960)

Applications Propylthiouracil N-β-D-Glucuronide Methyl Ester is a compound useful in organic synthesis.

Applications 2-​Ethyl-​2,​5-​dihydro-​4-​hydroxy-​3-​methyl-​5-​oxo-2-​furancarboxylic Acid Methyl Ester is an by-product intermediate formed during the synthesis of 4,5-Dimethyl-3-hydroxy-2(5H)-furanone (D473600), a fragrant compound that is a key indicator of maple syrup urine disease, a disorder affecting newborn children that is the result of its inability to properly metabolize Valine (V094205), Leucine (L330110) and Isoleucine (I820175). 4,5-Dimethyl-3-hydroxy-2(5H)-furanone is naturally found in fenugreek seeds, and is an odourant present in sherry wines.
References Blank, I., et al.: Prog. Flav. Prec. Stud., No vol. given, 103 (1993); Guerra, P. & Yaylayan, V.: J. Agr. Food Chem., 59, 4699 (2011); Mackenzie, D. & Woolf, L.: Brit. Med. J., 1, 90 (1959); Podebrad, F., et al.: J. Inh. Metab. Dis., 22, 107 (1999)

Applications Dichloroacetic Acid Methyl Ester is used in the preparation of telechelics and block copolymers through living radical polymerization.
References Keul, H., et. al.: Macromol. S., 19, 1 (1971)

Applications Used in the new synthesis of alkylsulphanylnaphthalenes and the synthesis and mesomorphic properties of novel naphthylisothiocyanates.
References Lauk, u., et al.: Helv. Chim. Acta, 68, 1406 (1985), Collina, S., et al.: Bioorg. Med. Chem., 8, 1925 (2000),

Applications (1S,2R,6R)-6-Acetoxy-2-((bis(benzyloxy)phosphoryl)oxy)-4-(ethoxycarbonyl)cyclohex-3-en-1-yl benzoate is an intermediate in the synthesis of Shikimate-3-phosphate (S357026), an substrate for 5-Enolpyruvoyl-shikimate-3-phosphate synthase (EPSPS), the target for the board-spectrum herbicide N-(phosphonomethyl)glycine(glyphosate).
References Mooney, C.A., et al.: J. Med. Chem., 57, 3154 (2014);

Applications (9Z)-Erythromycin A Oxime is a metabolite of Roxithromycin (R700850) in humans.
References Zhong, D. et al.: Drug Metab. Dispos., 28, 552 (2000)

Applications (Z)-3-Methylpent-2-en-4-yn-1-ol is used as a reagent in organic synthesis of many compounds including that of prolycopene which is a tangerine-colored tetra-Z-isomer of lycopene that is found in fruits of the tangerine tomato. Z)-3-Methylpent-2-en-4-yn-1-ol is also used in the synthesis of Leucosceptroids A and B which have potent antifungal properties.
References Pattenden, G., et al.: Tetrahedron Lett., 28, 5751 (1987); Guo, S., et al.: Angew. Chem. Int. Edit., 54, 1298 (2015);

Applications An intermediate in the preparation of heteropolycyclic quinolones.
References Dogan, J. et al.: Heterocycles, 41, 1659 (1995)

Applications Bis[2-(2-mercaptobenzoyl)hydrazide] 2,2'-Dithiobis-benzoic Acid is an intermediate used in the synthesis of N,N’-Bis(2-mercaptobenzoyl)hydrazide (B481825), which is a selective inhibitor of HIV-1 integrase. Has no other effect on other retroviral targets, including reverse transcriptase, protease, and virus attachement, and exhibits no detectable activity against human topoisomerases I and II at concentrations that effectively inhibit integrase.
References Neamati, N., et al.: J. Med. Chem., 45, 5661 (2003)

Applications Used in the preparation of labeled cocaine analogs.
References Carroll, F.I., et al.: J. Med. Chem., 35, 2497 (1992),

Applications 2,4-Dibromo Deuteroporphyrin IX Dimethyl Ester is an intermediate for the synthesis of Protoporphyrin IX Dimethyl Ester-d6 (P839127), which is the labelled version of Protoporphyrin IX P(P838900). Protoporphyrin IX (PPIX) is ubiquitously present in all living cells in small amounts as a precursor of heme and PPIX-based strategies have been used for cancer diagnosis and treatment. It can be used in biological study for role of protoporphyrin IX in skin photosensitivity, biliary stones, hepatobiliary damage, liver failure and cancer diagnosis and treatment in human.
References Sachar, M., et al.: J. Pharmacol. Exp. Ther., 356, 267-275 (2016)

Applications (S)-2-(Dimethoxymethyl)-1-pyrrolidinecarboxylic Acid 1,1-Dimethylethyl Ester is an intermediate in synthesizing Tilivalline (T440350), which is a metabolite from Klebsiella oxytoca. Tilivalline, is shown to be cytotoxin, and the key event causing Antibiotic-Associated Hemorrhagic Colitis.
References Mori, Sh., et al.: Tetrahedron, 47, No.27, 5051 (1991); Nagasaka, T., et al.: Tetrahedron Lett., 14, 1871 (1989);

Stability Moisture Sensitive
Applications An unknown impurity from the synthesis of Telmisartan (T017000).
References Wienen, W., et al.: Brit. J. Pharmacol., 110, 245 (1993), Neutel, J.M., and Smith, D.H.G.: Adv. Ther., 15, 206 (1998);

Applications N'-[(2-Chloro-5-thiazolyl)methyl]-N-nitro-carbamimidothioic Acid Methyl Ester-13C is an intermediate used in the synthesis of Clothianidin-d3,13C1(C588502), which is the isotope labelled analog of Clothianidin. Clothianidin is a neonicotinoid insecticide for use in food crops.
References Kamel, A., et al.: J. Agric. Food Chem., 58, 5926 (2010), Lynd, L., et al.: Energy Environ. Sci., 3, 1150 (2010), Cresswell, J., et al.: Ecotoxicology, 20, 149 (2011),

Applications (2E,6Z,8E)-2,6,8-Decatrienoic Acid Methyl Ester is an spilanthol (S681850) related amide found from Acmella ciliata.
References Martin, R., et al.: Phytochem., 23, 1781 (1984);

Applications 3’,4’-Dihydroxy-1-phenyl-2-butanone (cas# 17386-89-9) is a compound useful in organic synthesis.
References Strader, C., et al.: J. Biol. Chem., 266, 5 (1991),

Applications A coordination compound for treatment of cervix cancer.
References Jiang, M., et al.: Methods Mol. Biol., 292, 401 (2005), Fujii, T., et al.: Int. J. Oncol., 29, 541 (2006), Niu, X., et al.: Int. J. Gynecol. Cancer, 16, 743 (2006),

Applications (1S,2R)-1-((2S,3R,4S,6R)-3-Acetamido-4,6-diacetoxy-6-(methoxycarbonyl)tetrahydro-2H-pyran-2-yl)propane-1,2,3-triyl Triacetate is an intermediate in synthesizing 2-O-Methyl-α-D-N-acetylneuraminic Acid (M275400), which is a model compound for studies of binding of influenza virus hemagglutinin and metal ions.
References Sauter, N.K., et al.: Biochemistry, 28, 8388 (1989); Sharon, N., et al.: Science, 246, 227 (1989); Nagy, J.O., et al.: J. Med. Chem., 35 (23), (1992); Knibbs, R.N., et al.: J. Biol. Chem., 268 (25), 18524 (1993)

Applications 2,6-Dimethylnaphthalene is a polyaromatic hydrocarbon (PAH) environmental contaminant. 2,6-Dimethylnaphthalene is found in oil, coal and tar deposits and are produced by gasoline operating vehicles. It is a persistent environmental pollutant with carcinogenic and mutagenic activity.This compound is a contaminant of emerging concern (CECs)
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 Hays, M. et al.: Environ. Sci. Tech., 47, 14502 (2013); Lemieux, C. et al.: Environ. Toxicol. Chem., 27, 978 (2008); Gruger, E., et al.: Aquat. Toxicol., 5, 291(1984); Barnsley, E.: Appl. Environ. Microb., 54, 428 (1988); Miyachi N., et al.: Environ. Toxicol. Chem., 59, 1504 (1993)

Applications (-)-Galanthaminyl (-)-Camphanate (cas# 1025881-27-9) is a compound useful in organic synthesis.

Applications 2-Amino-4,6-dihydroxy-5-nitropyrimidine (cas# 80466-56-4) is a compound useful in organic synthesis.

Applications Isomer of (3R)-3-Hydroxy Quinine

Applications 5-Chloro-2-methoxy-benzoic Acid Methyl Ester-13C2,d6 (cas# 1794737-29-3) is a compound useful in organic synthesis.

Applications (2R,​3E)​-2,​4-​Dimethyl-​2-​[(1-​oxopropyl)​thio]​-​3,​5-​hexadienoic Acid Ethyl Ester is an intermediate in synthesizing (R)-(+)-Thiolactomycin (T350880). It is a natural product inhibitor of β-Ketoacyl-AcpM Synthase A (KasA). It inhibits the synthesis of mycolic acid which is a major cell wall component of Mycobacterium tuberculosis. Also an inhibitor of D-Aspartate oxidase (DDO).
References Kapilashrami, K., et al.: J. Biol. Chem., 288, 6045 (2013); Paneerselvam, V., et al.: J. Pharm. Res., 4, 4618 (2011); Katane, M., et al.: Biochimie, 92, 1371 (2010)

Applications Intermediate for the preparation of Isotope Labelled Tolmetin.

Applications 2-Fluoro-α-[(trimethylsilyl)oxy]benzeneacetonitrile is an intermediate in synthesizing 1-Cyclopropyl-2-(2-fluorophenyl)-2-hydroxy-ethanone (C989465), a useful synthetic intermediate in the synthesis of Prasugrel (P701150, HCl); an antiplatelet agent.
References Wiviott, S.D., et al.: Circulation, 116, 2923 (2007); Xu, X., et al. Faming Zhuanli Shenqing. CN 102718642 A 20121010. Oct 10, 2012; Wang, G., et al. Faming Zhuanli Shenqing. CN 101402556 A 20090408. Apr 8, 2009

Applications 2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine N-β-D-Glucuronide Triacetate is an intermediate in the synthesis of 2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine N-β-D-Glucuronide Sodium Salt which is a carcinogenic Sodium Salt, is a metabolite of 2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) (A617000).
References Turesky, R., et al.: Mutat. Res., 506 187 (2002), Sugimura, T., et al.: Cancer Sci., 95, 290 (2004),

Applications N-Methyl-6-(4-nitrophenoxy)-4-pyrimidinamine is an intermediate in the synthesis of N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-N'-[4-[[6-(methylamino)-4-pyrimidinyl]oxy]phenyl]urea (E926495), which is an inhibitor of RET, FLT3, KDR, c-Abl and c-Kit. Also, it prevent the growth of human thyroid cancer cells.
References Weisberg, E., et al.: Genes Cancer, 1, 1021-1032 (2010);

Applications 5β-Dihydrocortisol 21-O-(1-Ethoxy Ethyl) Ether-d6 is an isotope labelled intermediate in the synthesis of Tetrahydro Cortisone-d6 (T293377), which is a normal mammalian metabolite of Cortisone (C696500).
References Schneider, et al.: J. Biol. Chem., 183, 365 (1950), Barkemeyer, et al.: Appl. Microbiol., 8, 237 (1960),