Toxicologie

Applications Dydrogesterone (D826000) intermediate. Used in the preparation of 10α-steroids.

Applications D-2'-Deoxyribopyranosyl-3-guanylurea (α/β-Mixture) can be obtained from 5-Aza-2’-deoxy Cytidine (A796950) which can be used as cancer treatment, in particular to inhibit the growth of pancreatic endocrine tumor cell lines.
References Deng, T., et al.: Life Sci., 84, 311 (2009), Horne, H., et al.: Mol. Cancer Res., 7, 199 (2009), Zinner, R., et al.: Mol. Cancer Ther., 8, 521 (2009),

Applications A prototypical BCRP inhibitor. Inhibits the Bcrp1-mediated transport.
References Neville, K., et al.: Clin. Cancer Res., 10, 2525 (2004), Reardon, D., et al.: J. Clin. Oncol. 23, 9359 (2005), Pan, G., et al.: Drug Metab. Dispos., 35, 1165 (2007).

Applications N4-Anisoyl-2'-deoxycytidine (cas# 48212-99-3) is a useful research chemical.

Applications Glucocorticoid.

Applications Heterocyclic inhibitor of the RNA-dependent RNA polymerase enzyme transcribed by the Hepatitis C virus.
References Mashino, T., et al.: Bioorg. Med. Chem. Lett., 15, 1107 (2005), Liu, Y., et al.: Biochem., 45, 11312 (2006), Tedesco, R., et al.: J. Med. Chem., 49, 971 (2006),

Applications LY 364947, is a potent ATP-competitive inhibitor of Tgf-β signaling.
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 Ichida, J.K., et al.: Cell Stem Cell, 5, 491 (2009);

Applications (4S)-6-Chloro-1-(1-((S)-6-chloro-2-oxo-4-(trifluoromethyl)-2,4-dihydro-1H-benzo[d][1,3]oxazin-4-yl)pent-1-yn-3-yl)-4-(pent-1-yn-1-yl)-4-(trifluoromethyl)-1H-benzo[d][1,3]oxazin-2(4H)-one is an impurity of Efavirenz (E425000) which is a nonnucleoside HIV-1 reverse transcriptase inhibitor. Antiviral.
References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995),

Applications Diethyl α-Acetylglutarate is used in the preparation of furocoumarins as potential HIV-1 integrase inhibitors.
References Olomola, T.O., et. al.: Bioorg. Chem., 57, 1 (2014)

Applications 7-methoxy-4-phenyl-1,2-dihydroquinolin-2-one (cas# 30034-43-6) is a useful research chemical.

Applications 4-(1,1-Dimethylpropyl)-β-methylbenzenepropanol is a useful synthetic intermediate in the synthesis of Amorolfine Hydrochloride (A634170); a morpholine antifungal drug and topical solution for the treatment of toenail infections.
References Rotta, I., et al.: JAMA Dermatol., 149, 341 (2013); Espinel-Ingroff, A., et al.: Antimicrob. Agents Ch., 26, 5 (1984); Zhang, S., et al.: Faming Zhuanli Shenqing. CN 103288768 A 20130911. Sep 11, 2013

Applications Decapeptide LH-RH antagonist. Used in treatment of infertility.
References Strickley, R.G., et al.: Pharm. Res., 7, 530 (1990), Jung, G., et al.: J. Med. Chem., 35, 3942 (1992), Rabinovici, J., et al.: J. Clin. Endocrinol. Metab., 75, 1220 (1992), Devroey, P., et al.: Hum. Reprod., 13, 3023 (1998),

Applications (S)-1-Amino-3-chloro-2-propanol Hydrochloride is used in biological studies as an orally active male antifertility agent which is mediated by an effect on epididymal and vas deferens sperm.
References Coppola, J. A., et al.: Contraception, 9, 459 (1974);

Applications Bis(methylthio)gliotoxin (FR-49175) is an antiphagocytic metabolite.

Applications Isopropyl 2-Furoate is used in the preparation of heteroarenecarboxylates.
References Luo, Wenkun. et al., Org. Lett. 22, 2093-2098(2019);

Applications Marbofloxacin N-oxide is a metabolite of Marbofloxacin (M197000); a fluorinated quinolone antibacterial.
References Gruet, P., et al.: Vet. Rec., 140, 199 (1977); Lefebvre, H.P., et al.: J. Vet. Pharmacol. Ther., 21, 453 (1998); Schneider, M., et al.: J. Diary Sci., 87, 202 (2004)

Applications An impurity of Moxifloxacin (M745000).
References Tobin, C., et al.: J. Antimicrob. Chemother., 42, 278 (1998),

Applications N-Desdecanoyl, N-(8-Me-decanoyl) Daptomycin is an impurity of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial.
References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),

Applications 6-​Fluoro-​3-​[(trimethylsilyl)​oxy]​-2-​pyrazinecarboxamide is an intermediate in synthesizing T-705RTP (T003210), a derivative of T-705 (F103350) which has activity against the lethal H5N1 influenza A viruses. T-705RTP which has the triphosphate group, gets strongly inhibited by the influenza virus RNA polymerase activity in comparison with T-705RMP (T003202).
References Yousuke, F., et al.: Antimicrob Agent Chemother., 49, 981 (2005); Kiso, M., et al.: Proc. Natl. Acad. Sci. U.S.A., 107, 882 (2010);

Applications N'-Boc,N,N'-Desethylene Iso Gatifloxacin Anhydride with Diacetyl Borate is an impurity of Gatifloxacin (G250000), an antibacterial agent.
References Bauernfeind, A.: J. Antimicro. Chemother., 40, 639 (1997), Fukuda, H., et al.: Antimicrob. Ag. Chemother., 42, 1917 (1998),

Applications Nucleosides as antiviral agent for the treatment of influenza; broad-spectrum inhibitor of viruses in the Flaviviridae family.
References Sidwell, R.W., et al.: Appl. Microbiol., 22, 797 (1971), Allen, B., et al.: J. Med. Che,., 18, 721 (1976),

Applications (2E)-3-(2-Thiazolyl)-2-propenoic Acid is a useful synthetic intermediate. It is used as an intermediate for HIV-1 protease inhibitor.
References Baloglu, E., et al.: PCT Int. Appl. (2014), WO 2014085607 A1 20140605

Applications 6-Chloro-2-cyclohexyl-2,3-dihydro-1,3-dioxo-1H-isoindole-5-sulfonamide is an intermediate in the synthesis of Chlorexolone (C327080), a sulfonamide based antibiotic.

Applications Chloroquine N-oxide is a metabolite of Chloroquine (C379965), a standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labelling of MRP by quinoline-based photoactive drug IAAQ.
References Luthman, H., et al.: Nucleic Acids Res., 11, 1295 (1983), Vezmar, M., et al.: Biochem. Pharmacol., 56, 733 (1998), Krajewski, W.A., et al.: J. Biomol. Struct. Dyn., 16, 1097 (1999),

Applications 6-Methyl-3,6-diazabicyclo[3.1.1]heptane is a useful research chemical.

Applications Dibenzyloxy Tenofovir is an intermediate in the synthesis of Tenofovir Dibenzyloxy Isopropyl Carbamate (T018545); Acyclic phosphonate nucleotide analogue; reverse transcriptase inhibitor. Used as an anti-HIV agent. Antiviral.
References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997), Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007)

Applications BCX 4430 is an antiviral drug, an adenosine analog). It is developed by BioCryst Pharmaceuticals with funding from NIAID, originally intended as a treatment for Hepatitis C, but subsequently developed as a potential treatment for deadly filovirus infections such as Ebola virus disease and Marburg virus disease.
References Warren, T., et al.: Nature, 508, 7496 (2014); Kamat, S., et al.: Biochem., 52, 7366 (2013)

Applications Levamisole Phosphate is a compound used to study anthelmintic resistance status in Brazilian cattle.
References Soultello, R., et al.: Vet. Parasitol., 148, 360 (2007);

Applications 4-Acetylbenzenesulfonamide is a useful synthetic intermediate, and is also part of a group of sulfonamide derivatives that have potential to be carbonic anhydrase inhibitors.
References Carotti, A., et al.: Quant. Struct.-Act. Rel., 8, 1 (1989); Singh, P., et al.: Org. Chem.: An Indian Journal, 4, 540 (2008)

Impurity Entecavir EP Impurity C
Applications 8-Hydroxy Entecavir is an impurity of Entecavir (E558900), an oral antiviral drug used in the treatment of hepatitis B infection.

Applications Denatonium Benzoate Hydrate is a stimulant of the bitter taste receptors which allows for maintenance of the airways. Bronchodilator.
References Langtry, H.D., et al.: Drugs, 56, 273 (1998); Desphamde, D. et al.: Nat Med., 16, 1299 (2010); Meyerhof, W. et al.: Chem. Senses., 35, 157 (2010);

Applications N-4-(2,2,2-Trifluoroacetamido) Emtricitabine O-2,2,2-Trifluoroacetic Anhydride is an intermediate used in the synthesis of Emtricitabine Triphosphate Triethylammonium Salt (E525075), which is a metabolite of (-)-Emtricitabine (E525000).
References Barditch-Crovo, P., et al.: Antimicrob. Agents Chemother., 45, 2733 (2001); Ray, A., et al.: Antivir .Ther., 10, 451 (2005); Borroto-Esoda, K., et al.: Antivir. Ther., 11, 377 (2006)

Applications Rilpivirine Amadori rearrangement Product II is an impurity of Rilpivirine(R509800) which is a novel non-nucleoside reverse transcriptase inhibitor. Rilpivirine seems to be well tolerated with less CNS disturbance than Efavirenz, and has non-teratogenic potential. An anti-HIV agent.
References Sun, et al.: J. Med. Chem., 41, 4648

Applications (4S)-Efavirenz 2-Desoxo-2-methyl is an analog of Efavirenz (E425000); a nonnucleoside HIV-1 reverse transcriptase inhibitor and antiviral agent.
References Young, S.D., et al.: Antimicrob. Ag. Chemother., 39, 2602 (1995)