Hormones in Recombinant Proteins

Applications The hydrophilic metabolite of Dexamethasone (D298800). References Draper, R., et al.: Drug Res., 32, 317 (1982), Watkins, P., et al.: Clin. Pharmacol. Ther., 52, 265 (1992), Yamamoto, N., et al.: J. Clin. Oncol., 18, 2301 (2000), Slaviero, K., et al.: Br. J. Clin. Pharmacol., 57, 44 (2004),

Applications 6α,9α-Difluoroprednisolone 17-Acetate, is an impurity of Difluprednate (D445925), which is shown to have antiinflammatory activity. References Vitali, R., et al.: J. Med. Chem., 20, 853 (1977);

Applications Cyproterone Acetate-d3, is the labeled analogue of Cyproterone Acetate (C989100), which combined with estrogen it is used in the treatment of acne. References Moltz, L., et al.: Contraception, 21, 393 (1980), Hammerstein, J., et al.: J. Steroid Biochem., 29, 591 (1983)

Applications Ulipristal is a selective progesterone receptor modulator. Ulipristal is used as an emergency contraceptive. References Gronemeijer, H., et al.: J. Steroid Biochem., 40, 271 (1991), Spitz, I., et al.: Contraception, 48, 403 (1993), Conneely, O., et al.: Steroids, 68, 771 (2003), Chwalisz, K., et al.: Endocr. Rev., 26, 423 (2005),

Stability Hygroscopic Applications Sodium 17beta-Estradiol-2,4,16,16-d4 3-Sulfate (Stabilized with TRIS, 50% w/w) (CAS# 352431-50-6) is a useful isotopically labeled research compound.

Applications Labelled N-Methylepinephrine, the N-methylated analogue of the sympathomimetic hormone Epinephrine (E588585). Recent studies suggest that N-Methylepinephrine may be synthesized from Epinephrine by phenylethanolamine N-methyltransferase present in the brain. References Kajita, M. et al.: Nip. Iyo Masu Sup. Gak. Kon., 19, 107 (1994); Plummer, C.J. et al.: Eur. J. Med. Chem., 148, 481 (1988);

Applications Testosterone Heptanoate-6,6,7,7,7-d5 (CAS# 1263095-31-3) is a useful isotopically labeled research compound.

Applications (E)-4-Hydroxy Tamoxifen-d5 is an labelled metabolite of Tamoxifen (T006000). A hydroxylated analogue of Tamoxifen with anti-estrogenic properties. References Muerdter, T.E., et al.: Clin. Pharmacol. Therapeut., 89, 708 (2011); Dorchies, O. M., et al.: Am. J. Pathol., 182, 485 (2013);

Applications Bazedoxifene N-Oxide is a metabolite of the selective estrogen receptor modulator, Bazedoxifene (B129250) References Chandrasekaran, A. et al.: Drug Metab. Dispos., 37, 1219 (2009);

Applications Juvenile Hormone B 3 is a sesquiterpenoid produced by the larval ring gland and adult corpus allatum (CA) of Drosophila melanogaster. Juvenile hormones regulate development, reproduction, diapause, and polyphenisms. References Wang, Ch., et al.: Gen. Comp. Endocr., 176, 347 (2012); Bendena, W.G., et al.: Gen. Comp. Endocr., 172, 56 (2011); Wyatt, G., Davey, K.: Adv. Insect Physiol., 26, 1 (1996); Nijhout, H.: Insect Hormones (Princeton Univ. Press, Princeton) (1994)

Applications Glycochenodeoxycholic Acid-d5 (G641257) derivative.

Applications 5α-Cholestan-3β-ol-d7 is the isotope labelled analog of 5α-Cholestan-3β-ol. 5α-Cholestan-3β-ol is a carbon stanol formed from biohydrogenation of Cholesterol (C432501) in the gut. References Serizawa, S., et al.: J. Biochem., 92, 547 (1982);

Impurity Clobetasol Propionate EP Impurity D Applications 21-Chloro-9-fluoro-11β,17-dihydroxy-16β-methylpregn-4-ene-3,20-dione 17-Propionate (Clobetasol Propionate EP Impurity D) is an impurity of Clobetasol 17-Propionate (C583500), an topical corticosteroid with anti-inflammatory properties. References Olsen, E.A., et al.: J. Am. Acad. Dermatol., 15, 246 (1986),

Applications (3β)-24-Bromo-3-[(tert-butyl)dimethylsilyloxy]-chol-5-ene is a reactant used in the preparation of series of cholesterol side-chain analogs used in studies of the ω-regiospecificity of Mycobacterium tuberculosis cholesterol metabolizing cytochrome P 450 enzymes CYP124A1, CYP125A1 and CYP142A1. References Johnston, J. et al.: Bioorg. Med. Chem., 20, 4064 (2012)

Applications Labelled Melengestrol acetate (M215352). Orally active progestational steroid. Progestogen; growth promotant. References Patton, M., et al.: Zoo Biol., 26, 311(2007), Sellin, M., et al.: Environ. Toxicol. Chem., 28, 2443 (2009), Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009), Sanseverino, J., et al.: Toxicol. Sci., 107, 122 (2009),

Pancreatic derived factor, also known as FAM3B, is an islet-specific secreted cytokine specifically expressed at high levels in the islets of Langerhans of the

Applications 17-epi-Testosterone-d3 is the labelled analog of 17-epi-Testosterone.Testosterone (T155000) and epitestosterone (T155005) are endogenous steroids that differ in the configuration of the hydroxyl-bearing carbon at C-17. Testosterone is the predominant male sex hormone, whereas the role of epitestosterone is largely unclear. In humans, both androgens are excreted mainly as glucuronide conjugates. References Wudy, S., et al.: Steroids, 66, 759 (2001), Kootstra, P., et al.: Anal. Chim. Acta., 586, 82 (2007), Sten, T., et al.: Drug Metab. Dispos., 37, 417 (2009),

Applications Isotope labelled 19-Norandrosterone is the oxidized byproduct of Nandrolone (N315000), an anabolic steroid that is present naturally in the human body. References Jiang, J.Q., et al.: J. Food. Sci., 77, 63 (2012); Delgadillo, M.A., et al.: J. Chromatograph. Anal. Technol. Biomed. Life. Sci., 897 (2012);

Applications Norgestimate-d3 is the labeled Norgestimate, a progestogen. In combination with estrogen as oral contraceptive. References Hahn, D.W., et al.: Contraception, 16, 541 (1977); Weintraub, H.S., et al.: J. Pharm. Sci., 67, 1406 (1978)

Applications An intermediate of Deflazacort (D228975), a systematic corticosteroid. References Nathansohn, G. et al.: Steroids, 13, 365 (1969); Nathansohn, G., et al.: J. Med. Chem., 10,799 (1967), Schiatti, P., et al.: Arzneim. Forsch., 30, 1543 (1980),

Applications A labelled metabolite of Estradiol (E888000). References Fishman, H.G, et al.: Biochemistry, 8, 4304 (1969), Ryan, Sugar, J., et al.: J. Clin. Endocrinol. Metab., 50, 137 (1980), Numazawa, M., et al.: Steroids, 38, 149 (1981), Travis, R., et al.: Breast Cancer Res., 5, 239 (2003),

Applications A labelled Cholic Acid (C432600) derivative used as a component in cell lysis buffers. References Tuangtong, R. et al.: Dermatol. Surg., 36, 899 (2010); Araki, Y. et al.: Scand. J. Gast., 36, 533 (2001);

Applications A glucocorticoid anti-inflammatory agent. Regulates T cell survival, growth, and differentiation. Inhibits the induction of nitric oxide synthase. References Wershil, B.K., et al.: Int. Arch. Allergy Immunol., 107, 323 (1995), Riccardi, C., et al.: Cell Death Diff., 6, 1182 (1999), Llanos, S.L. and Roldan, A.: Bio Cell, 23, 29 (1999)

Impurity Megestrol Acetate EP Impurity G Applications (2β)-Methyl Megestrol Acetate (Megestrol Acetate EP Impurity G) is a related impurity in Megestrol acetate (M208050). References Schneider, F., et al.: Helv. Chim. Acta, 56, 2396 (1973), Aisner, J., et al.: Semin. Oncol., 15, 68 (1988), Krischenowski, D., et al.: Steroids, 58, 278 (1993), Bratoeff, E., et al.: Chem. Pharm. Bull., 51, 1132 (2003),

Applications Sodium salt of Dexamethasone β-D-Glucuronide is a potential prodrug for colonic delivery of the antiinflammatory corticosteroid Dexamethasone. References Fotsis, T., et al.: J. Steroid Biochem., 14, 457 (1981), Choi, M., et al.: Steroids, 65, 54 (2000); Haeberlin, B. et al.: Pharm Res., 10, 1553 (1993);

Applications Labelled Cyproterone (C989090). An antiandrogen, suppresses Testosterone and its metabolites. Derivatives of Cyproterone are administered to patients suffering from hypersexuality and to help facilitate the sexual transformation of male-to-female transsexuals. References Gracia, T., et al.: Toxicol. App. Pharmacol., 225, 142 (2007), Ahlin, G., et al.: J. Med. Chem., 51, 5932 (2008), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010), Bovee, T., et al.: J. Steroid Biochem. Mol. Biol., 118, 85 (2010),

Applications Sodium Cholesterol-25,26,26,26,27,27,27-d7 Sulfate is a useful isotopically labeled compound of Cholesterol 3-Sulfate Sodium Salt (C432500)

Applications (3β)-3-O-tert-Butyldimethylsilyl-cholest-5-ene-3,24-diol is a reactant used in the preparation of series of cholesterol side-chain analogs used in studies of the ω-regiospecificity of Mycobacterium tuberculosis cholesterol metabolizing cytochrome P 450 enzymes. It is used in the preparation of (25S)-Δ7-dafachronic acid, (25S)-Δ4-dafachronic acid, (25S)-dafachronic acid, and (25S)-cholestenoic acid. References Johnston, J. et al.: Bioorg. Med. Chem., 20, 4064 (2012); Martin, R. et al.: Org. Biomol. Chem., 6, 4293 (2008)

Applications Gibberellin A7 is an plant hormone that was isolated from culture filtrates of the fungus Gibberella fujikuroi. Gibberellin A7 was shown to promote the growth and elongation of cells. References Cross, B.E., et al.: Tetrahedron., 8, 451 (1962); Meijon, M., et al.: J. Plant. Growth. Regulat., 30, 74 (2011); Ward, D.A., et al.: Phytochem., 71, 2010 (2010);

Insulin-1 Protein, Mouse, Recombinant (His & Myc) is expressed in Yeast.

Applications Taurocholic Acid-d8 Sodium Salt is the isotope labelled analog of Taurocholic Acid Sodium Salt; a bile acid with potential tumor-promoting and tumor-initiating activities in the glandular stomach mucosa of F344 rats. References Furihata, C., et al.: Jpn. J. Cancer Res., 78, 32 (1987)

Applications 21-Dehydro Betamethasone is an impurity of Betamethasone (B327000), a corticosteroid used as an anti-inflammatory agent. References Chen, B., et al.: Steroids, 74, 30 (2009); Li, M., et al.: J. Pharm. Sci., 98, 894 (2009); Xiong, Y., et al.: J. Pharm. Biomed. Anal., 49, 646 (2009);

Applications A labelled steroid hormone with weak androgenic activity. It is metabolized from Testosterone (T155000) in the liver and is used in doping analysis to detect testosterone misuse. Controlled Substance. References Park, J., et al.: J. Anal. Toxicol., 14, 66 (1990),; Palonek, E., et al.: J. Steroid Mol. Biol., 55, 121 (1995); Aguilera, R., et al.: Clin. Chem. 47, 292 (2001); Flenker, U., et al.: Steroids, 73, 408 (2008); Saudan, C. et al.: Steroids, 70, 179 (2005);

Applications An injectable gonadotropin-releasing hormone (GnRH) super-agonist (also known as an LHRH agonist). Used in treatment of precocious puberty and commonly used in veterinary medicine to induce ovulation in mares. References Linde, R. et al.: Engl. J. Med., 305, 663 (1981); Manasco, P.K. et al.: J. Pediatr., 115, 105 (1989); Johnson, C.A. et al.: J. Anim. Sci., 81, 1300 (2003); Farquhar, V.J. et al.: J. Am. Vet. Med. Assoc., 218, 749 (2001);

Applications A labelled progesterone receptor antagonist with partial agonist activity. Abortifacient. References Healy, D.L., et al.: J. Clin. Endocrinol. Metab., 57, 863 (1983), Rauch, M., et al.: Eur. J. Biochem., 148, 213 (1985), Baulieu, E.E., et al.: Science, 245, 1351 (1989), Brogden, R.N., et al.: Drugs, 45, 384 (1993)

Prolactin Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag.

Procalcitonin/CALCA Protein, Human, Recombinant (mFc) is expressed in HEK293 mammalian cells with mFc tag.

Applications Diflucortolone-d3 (D445617) derivative. A glucocorticoid.

Applications Controlled substance (anabolic steroid). Labelled prohormone of Trenbolone (T719000). References Schanzer, W., et al.: Clin. Chem., 42, 1001 (1996), Kicman, A., et al.: Br. J. Pharmacol., 154, 502 (2008), Fragkaki, A., et al.: Steroids, 74, 172 (2009),

Adiponectin Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag.

Applications A metabolite of Triamcinolone acetonide. References Edsbacker, S., et al.: Drug Metab. Dispos., 11, 590 (1983), Szefler, S., et al.: Eur. J. Clin. Pharmacol., 30, 323 (1986), Hansel, T., et al.: J. Immunol. Methods, 145, 105 (1991), Argenti, D., et al.: J. Clin. Pharmacol., 39, 695 (1999),

Applications A common enironmental pollutant showing weak estrogenic effects. Has been shown to cause harm to the male reproductive system of vertebrates in particular among aquatic species where gonadal intersex, altered sex ratios, and reduced gonad size has been observed. References Nishio, E., et al.: Biosci., Biotechnol., Biochem., 69, 1226 (2005), Barber, L., et al.: Aquatic Toxicol., 82, 36 (2007), Vajda, A., et al.: Environ. Sci. Technol., 42, 3407 (2008),

Impurity Betamethasone EP Impurity C Applications (16β)-17,21-Dihydroxy-16β-methyl-pregna-1,4,9(11)-triene-3,20-dione (Betamethasone EP Impurity C) is used in biological studies to perform preclinical characterization of VBP15, a novel anti-inflammatory delta 9,11 steroid. This compound is also used in analytical studies to determine the stability from reversed-phase high performance liquid chromatography (RP-HPLC) to separate low levels of dexamethasone and other related compounds from betametasone, which is an active pharmaceutical ingredient. References Reeves, E.K.M., et al.: Bioorg., Med. Chem., 21, 2241 (2013), Xiong, Y., et al.: J. Pharm. Biomed. Anal., 49, 646 (2009)

Applications Labelled 17α-Hydroxyprogesterone (H952330). 17α-Hydroxy Progesterone is a metabolite of Progesterone. It was isolated from adrenal glands. References Pfiffner, N., et al.: J. Biol. Chem., 132, 459 (1940), Florey, K., et al.: Anal. Profiles Drug Subs.,4, 209 (1975),

Applications Chlormadinol Acetate-d3, is the labeled analogue of Chlormadinol Acetate (C343460), the active metabolite of Chlormadinone acetate (CMA) (C343500). References Vaitukaitis, J., et al.: J. Clin. Endocrinol. Metab., 33, 988 (1971), Handy, R., et al.: Drug Metab. Disposition., 2, 214 (1974), Fiet, J., et al.: Steroids, 66, 609 (2001),

Applications Quinbolone is an anabolic steroid. Quinbolone is a cyclopentenyl ether derivative of Boldenone (B675100) which is also its active metabolite. Quinbolone shows weak androgenic activity. References Balestreri, R. et al.: Arch. Maragl. Patol. Clin., 22, 369 (1966); Galletti, F. et al.: Steroids, 18, 39 (1971);

Applications Labelled Medroxyprogesterone, an orally active progestogen used in hormone replacement therepy (HRT), in the past has been used as a component of oral contraceptives. References Pan, Q., et al.: Mol. Hum. Reprod., 13, 797 (2007), Matsson, P., et al.: J. Pharmacol. Exp. Ther., 323, 19 (2007), Jukosky, J.A., et al.: Bull. Environ. Contam. Toxicol., 81, 230 (2008), Cherkasov, A., et al.: J. Med. Chem., 51, 2047 (2008),

Applications Testololactone, is the derivative of Testolactone (T154800), which is an antineoplastic agent that is a derivative of progesterone and is used to treat advanced stage breast cancer. References Dunkel, L.: Mol. Cell. Endocrinol., 254, 207 (2006); Eugster, E. A.: Treat. Endocrinol., 3, 141 (2004); Holbeck, S.L. et al.: Mol. Cancer Therap., 9, 1451 (2010);

Applications The minor metabolite of Deflazacort. References Bernareggi, A., et al.: J. Pharma. Biomed. Anal., 5, 177-81 (1987), Assandri, A., et al.: Xenobiotica, 13(3), 185 (1983), Martinelli, E., et al.: Drug Metab. Dispos., 7, 335 (1979),

Applications Exemestane-13C,D3 is the labeled analogue of Exemestane (E957000), an antineoplastic (hormonal). References Giudici, D., et al.: J. Steroid Biochem., 30, 391 (1988), Evans, T.R.J., et al.: Cancer Res., 52, 5933 (1992), Zilembo, N., et al.: Brit. J. Cancer, 72, 1007 (1995)

Iron-regulatory hormone that acts as an erythroid regulator after hemorrhage: produced by erythroblasts following blood loss and mediates suppression of

Impurity Raloxifene EP Impurity D Applications LY 88074 is a selective estrogen receptor modulator (SERM). LY 88074 has potential use in the treatment of estrogen deprivation syndrome. References Dai, S.Y. et al.: Proc. Nat. Acad. Sci. USA, 105, 7171 (2008); Dai, S.Y. et al.: Biochemistry, 48, 9668 (2009);

Hormone that seems to suppress insulin ability to stimulate glucose uptake into adipose cells.

Applications 4-Hydroxy Estrone 1-N3-Adenine is an estrogen metabolite formed with DNA which can lead to the mutations that initiate breast, prostate, and other types of cancer. The N3Ade depurinating adducts could serve as biomarkers to predict the risk of breast cancer. References Chakravarti, D., et al.: Mutat. Res., 456, 17 (2000), Liehr, J., et al.: Endocr. Rev., 21, 4054 (2000), Chakravarti, D., et al.: Oncogene, 20, 7945 (2001), Cavalieri, E., et al.: Chem. Res. Toxicol., 14, 1041 (2002),

Applications Dacuronium Bromide is a metabolite of neuromuscular blocking agent Pancuronium (P178500) with much weaker activity. References Marshall, I.G. et al.: Br. J. Anaesth., 55, 703 (1983); Norman, J. et al.: Br. J. Anaesth., 43, 313 (1971); Durant, N.N. et al.: J. Pharm. Pharmacol., 31, 831 (1979);

Applications Labelled 5β-Pregnane-3α,20α-diol, a metabolite of Progesterone (P755900). References Beall, et al.: Biochem. J., 31, 35 (1937); Okuda, A. et al.: J. Biol. Chem., 259, 7519 (1984); Russell, D. et al.: Biochemistry, 31, 4737 (1992); Kondo, K. et al.: Eur. J. Biochem.; 219, 357 (1994); Westerbacka, J. et al.: J. Clin. Endocrinol. Metab., 88, 4924 (2003);

Applications Testosterone and epitestosterone are endogenous steroids that differ in the configuration of the hydroxyl-bearing carbon at C-17. Testosterone is the predominant male sex hormone, whereas the role of epitestosterone is largely unclear. In humans, both androgens are excreted mainly as glucuronide conjugates. References Wudy, S., et al.: Steroids, 66, 759 (2001), Kootstra, P., et al.: Anal. Chim. Acta., 586, 82 (2007), Sten, T., et al.: Drug Metab. Dispos., 37, 417 (2009),

Applications 2-Hydroxy-estrone-6-N3-adenine is a depurinating adduct that is created by the interaction of specific metabolites of estrogens in the body with DNA. Unfortunately, these adducts are endogenous initiators of various human cancers, such as breast & prostate. References Yang, L., et al.: Prostate, 69, 41 (2009); Zahid, M., et al.: Chem. Res. Toxicol., 19, 164 (2006); Zhang, Y., et al.: Metabol. Clin. Exp., 56, 887 (2007)