Toxicology

Applications N-Deethoxymethyl Chlorfenapyr is a primary metabolite of Chlorfenapyr (C428500). Chlorfenapyr is a halogenated pyrrole based pro-insecticide. Chlorfenapyr functions by metabolizing into an active insecticide after entering the host. Chlorfenapyr is used primarily as a means of pest control on cotton.
References Lovell, J.B. et al.: Bright. Crop Prot. Pests Dis., 1, 37 (1990); Wier, A.T. et al.: J. Agric. Entemol., 11, 311 (1994); Black, B.C. et al.: Pest. Biochem. Physiol., 50, 115 (1994); Albers, P. H., et al.: Environ. Toxicol. Chem., 25, 438 (2006)

Applications A new salt of HMG-CoA reductase inhibitor.

Applications Isotope Labelled 1-Cyclopropyl-8-ethoxy-6,7-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acid is an impurity in the synthesis of Moxifloxacin (M745000), a fluorinated quinolone antibacterial.
References Woodcock, J.M., et al.: Antimicrob. Ag. Chemother., 41, 101 (1997), Stass, H., et al.: Antimicrob. Ag. Chemother., 42, 2060 (1998)

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-(5-Bromothiophen-2-yl)benzonitrile (CAS# 415718-60-4) is a useful research chemical compound.

Applications Metopimazine (MPZ) is used to prevent emesis during chemotherapies. Antiemetic.
References Catz, P., et al.: Int. J. Pharm., 58, 93 (1990), Sato, K., et al.: J. Pharm. Sci., 80, 104 (1991), Herrstedt, J., et al.: Cancer Chemother. Pharmacol., 33, 53 (1996), Sigsgaard, T., et al.: J. Clin. Onc., 19, 2091 (2001),

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 The R-enantiomer of Baclofen (B108000) metabolite.

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 Aprindine is a long-acting antiarrhythmic agent, effective when administered orally or intravenously in the treatment of ventricular arrhythmias of varying etiologies.
References Danilo, P. Jr., et al.: Am. Heart. J., 97, 119 (1979); Atarashi, H., et al.: Circulation. J., 66, 553 (2002);

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 Bivalirudin 1-11 Fragment is an impurity of Bivalirudin, a direct thrombin inhibitor acting as an anticoagulant through inhibition of the enzyme thrombin.
References Bertrand, O. et al.: Am. J. Cardio., 110, 599 (2012); Patti, G. et al.: Am. J. Cardio., 110, 478 (2012)

Applications Rosuvastatin Methyl Ester is an impurity of Rosuvastatin (R700500) in the pharmaceutical dosage forms under forced degradation conditions.
References Lennernas, H., et al.: Clin. Pharmacokinet., 32, 403 (1997), Kivisto, K., et al.: Br. J. Clin. Pharmacol., 46, 49 (1998), Lan, K., et al.: J. Pharm. Biomed. Anal., 44, 540 (2007),

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 An optically active metabolite of Tramadol.
References Garrido, M., et al.: J. Pharmacol. Exp. Ther., 305, 710 (2003), Pedersen, R., et al.: Eur. J. Clin. Pharmacol., 62, 513 (2006),

Impurity Beclomethasone Dipropionate EP Impurity I
Applications (16β)-16-Methyl-17,21-bis(1-oxopropoxy)pregna-1,4,9(11)-triene-3,20-dione (Beclomethasone Dipropionate EP Impurity I) is an impurity of Beclomethasone (B131000), a glucocorticoid. Used in chronic asthma and allergic rhinitis. Antiallergic, antiasthmatic (inhalant). Anti-inflammatory (topical).
References Malfitan, V.A., et al.: Clin. Ther., 4, 472 (1982), Rao, M., et al.: J. Asthma, 19, 21 (1982), Small, P., et al.: Ann. Allergy, 49, 127 (1982), Brogden, R.N., et al.: Drugs, 28, 99 (1984),