Hormones in Recombinant Proteins

Applications NN703 (Tabimorelin) is an orally active growth hormone (GH) secretagogue intended for use as an alternative to daily injections of GH. In vitro studies in human liver microsomes have indicated that NN703 is a mechanism-based inhibitor of CYP3A4. References Fabre, G., et al.: Biochem. Pharmacol., 37, 4389 (1988), Thummel, K., et al.: Clin. Pharmacol. Ther., 59, 491 (1996), Yu, D., et al.: J. Clin. Pharmacol., 39, 1203 (1999),

Applications Pralmorelin is a growth hormone secretagogue that acts on the pituitary gland and the hypothalamus to stimulate and amplify pulsatile growth hormone release. References Howard, A. D., et al.: Science, 273, 974 (1996)

Applications A labelled progestogen with low androgenic potency. References Viinikka, L., et al.: Eur. J. Clin. Pharmacol., 15, 349 (1979), Bergink, E.W., et al.: J. Steroid Biochem., 14, 175 (1981)

Applications Labelled 4-Methoxyestrone (M226135). An endogenous estrogen metabolite, risk-factor for development of breast cancer. References Beral, V., et al.: Lancet, 362, 419 (2003), Nelson, R., et al.: Clin. Chem., 50, 373 (2004), Malekinejad, H., et al.: J. Agric. Food Chem., 54, 9785 (2006),

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

Applications (3α)-Allopregnanolone Sulfate is the sulfate conjugate of (3α)-Allopregnanolone (A547100), a metabolite of progesterone and potent positive modulator of GABAA receptors. References El-Etr, M. et al.: Brain Res., 790, 334 (1998); Hauser, C.A.E. et al.: Eur. J. Pharmacol. Mol. Pharmacol. Sec., 289, 249 (1995);

Applications Androstenedione (A637550) analog, an aromatase inhibitor. References Marsh, D.A., et al.: J. Med. Chem., 28, 788 (1985),

Applications Clobetasol Propionate Impurity E is an impurity of Clobetasol (C583490), which is a topical corticosteroid. Glucocorticoid; anti-inflammatory. References Olsen, E.A., et al.: J. Am. Acad. Dermatol., 15, 246 (1986),

Applications The major metabolite of Boldenone, an anabolic steroid. References Fotsis, T., et al.: J. Steroid Biochem., 28, 203 (1987), Song, Y., et al.: Arch. Pharm. Res., 23, 599 (2000), Buiarelli, F., et al.: Anal. Chim. Acta, 526, 113 (2004), Poelmans, S., et al.: Food Addit. Contam., 22, 808 (2005),

Stability Hygroscopic Applications An active agent in the preparation of a pharmaceutical for the treatment of asthma or other respiratory diseases.

Applications A labelled metabolite of Pregnenolone (P712200). References Kramer, R., et al.: J. Steroid Biochemi., 18, 715 (1983), Hiwatashi, A., et al.: J. Biochem., 98, 619 (1985), Eiichi, T., et al.: J. Pharmacol. Sci., 95, 140 (2004),

Applications Ulipristal Acetate-d3, is the labeled analogue of Ulipristal Acetate (U700812), a selective progesterone receptor modulator. Ulipristal acetate is used during pregnancy. 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);

Impurity Fluocinolone Acetonide EP Impurity I Applications 14,15-Dehydro Fluocinolone Acetonide is an impurity of Fluocinolone Acetonide (F455800); a glucocorticoid and anti-inflammatory agent. References Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964); Emerson, M.V., et al.: BioDrugs, 21, 245 (2007)

Applications 17a-Oxa-D-homo-5β-androst-1-ene-3,17-dione is a metabolite in the urine of men following treatment with Δ1-testololactone, which is an idiopathic oligospermic infertility. Also, it is derived from Androstenedione (A637550), which is a testosterone precursor and metabolite with androgenic activity. Controlled substance (anabolic steroid). References Yaeger, R. L., et al.: Drug Metab. Dispos., 13, 107-109 (1985); Walker, V.R., et al.: Anal. Biopchem., 234, 194 (1996), King, D.S., et al.: J. Am. Med. Assoc., 281, 2020 (1999)

Applications 4-Hydroxy Estradiol 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),

Stability Isomerizes rapidly in Benzene, Chloroform, and Ether.Keep Shielded from light. Applications A synthetic, nonsteroidal estrogen.Recomended solvents are DMSO, DMF and ethanol, even in these solvents do not store in solution for any prolonged period of time. References White, W. A. et. al.: J. Agric. Food Chem. 19(2), 388-390 (1971).

Impurity Fulvestrant Impurity E; Applications Fulvestrant (F862500) impurity E.

Applications A derivative of dehydrochloromethyltestosterone. Metabolite of anabolic steroids. References Rendic, S., et al.: J. Chromatogr. 735, 73 (1999)

Relaxin is an ovarian hormone that acts with estrogen to produce dilatation of the birth canal in many mammals.

Glycoprotein hormones alpha chain Protein, Canine, Recombinant (His) is expressed in Yeast.

Applications The labelled epimer of Medroxyprogesterone acetate (M203560). Progesterone impurity. References Tang, M., et al.: Endocrinol., 151, 1320 (2010), Lee, K., et al.: Mol. Cell. Endocrinol., 319, 109 (2010), Rodgers, A., et al.: Chem., Res. Toxicol., 23, 724 (2010), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010),

Resistin is an adipocytokine, which has been studied for its role in insulin resistance and recently in inflammation.

Applications Stable labelled metabolite of Ursodeoxycholic Acid, which is used as an anticholelithogenic.

Applications Testosterone-2,2,4,6,6-d5 Heptanoate is a useful isotopically labeled compound of Testosterone Enanthate (T155080)

Applications 5,6-Dehydro-17α-dutasteride is an epimer of 5,6-Dehydro-17β-dutasteride (D229560) an impurity in the synthesis of Dutasteride (D735000), a dual inhibitor of 5α-reductase isoenzymes type 1 and 2; structurally related to Finasteride (F342000). Dutasteride is used in the treatment of benign prostatic hyperplasia. References Bakshi, R.K., et al.: J. Med. Chem., 38, 3189 (1995), Gisleskog, P.O., et al.: Brit. J. Clin. Pharmacol., 47, 53 (1999), Djavan, B., et al.: Expert Opin. Pharmacother., 6, 311 (2005),

Applications 4’-Hydroxy Dutasteride is an impurity of Dutasteride (D735000), a dual inhibitor of 5α-reductase isoenzymes type 1 and 2; structurally related to Finasteride (F342000). Dutasteride is used in the treatment of benign prostatic hyperplasia. References Bakshi, R.K., et al.: J. Med. Chem., 38, 3189 (1995), Gisleskog, P.O., et al.: Brit. J. Clin. Pharmacol., 47, 53 (1999), Djavan, B., et al.: Expert Opin. Pharmacother., 6, 311 (2005)

Chorionic Gonadotropin/CGA Protein, Human, Recombinant is expressed in HEK293 mammalian cells.

Applications Labelled Campesterol (C155360). A phytosterol, which may inhibit the intestinal absorption of cholesterol. References Fransen, H., et al.: J. Nut., 140, 1062 (2010), Kojoma, M., et al.: Plant Biotechnol., 27, 59 (2010), Orozco-Solano, M., et al.: J. Agric. Food Chem., 58, 7539 (2010),

Stability Hygroscopic Applications Analog of thyrotropin releasing hormone TRH, with pronounced CNS activity. Used in the treatment of spinocerebellar degeneration. References Yamamura, M., et al.: Jpn. J. Pharmacol., 53, 451 (1990), Iwasaki, Y., et al.: Neurol. Res., 19, 613 (1997), Kinoshita, K., et al.: CNS Drug Rev., 4, 25 (1998), Morikawa, S., et al.: J. Pharm. Biomed. Anal., 16, 1267 (1998),

CGRP induces vasodilation.

Applications An impurity of Finasteride (F342000).

Applications 6-keto Dexamethasone, is an impurity of Dexamethasone, a glucocorticoid used as an anti-inflammatory agent. Dexamethasone regulates T cell survival, growth, and differentiation. Dexamethasone inhibits the induction of nitric oxide synthase.

Applications Lynestrenol is an orally available progestogen hormone used in contraception to avoid hereditary angiodema as well as in treatment of ischemic stroke. References Saule, C. et al.: Clin. Exp. Allergy, 43, 475 (2013); Beraki, S. et al.: PLoS One., 8, e69233 (2013);

Applications Alphadolone or Alfadolone (INN) is a neuroactive steroid with hypnotic effects. Alphadolone is one of the components of Althesin. References Harrison, N., et al.: J. Pharmacol. Exp. Ther., 241, 346 (1987), Serrao, J., et al.: Anesthesiology, 70, 780 (1989), Mistry, D., et al.: Exp. Physiol., 75, 199 (1900),

Applications A Dexamethasone Dipropionate metabolite. References Miyachi, Y., et al.: Steroids, 52, 137 (1988), Soh H., et al.: Brit. J. dermatol., 125, 73 (1991), Civiale, C., et al.: J. Ocul. Pharmacol., Thera., 20, 75 (2004),

Functions as a heterodimeric glycoprotein hormone with GPHA2 able to bind and activate the thyroid-stimulating hormone receptor (TSHR), leading to increased

Applications A metabolite of Tibolone. A synthetic steroid with weak estrogenic, androgenic and progestogenic activity. A pharamceutical used in the treatment of menopausal syndrome. References Belman, S., et al.: Cancer Res., 32, 450 (1972), Shirahashi, H., et al.: Chem. Pharm. Bull., 41, 1664 (1993), Hoyte, R., et al.: Steroids, 58, 13 (1993), Sandker, G., et al.: Xenobiotica, 24, 143 (1994), Colombo, D., et al.: Eur. J. Med. Chem., 40, 69 (2005),

Applications A metabolite of Desogestrel. References Back, D., et al.: Br. J. Clin. Pharmacol., 26, 23 (1988), Wienkers, L., et al.: Drug Metab. Dispos., 1990, 24, 610 (1990), Bourrie, M., et al.: J. Pharmacol. Exp. Ther., 277, 321 (1996), Ono, S., et al.: Xenobiotica, 26, 681 (1996),

Applications Glycolithocholic-2,2,4,4-d4 Acid (CAS# 2044276-16-4) is a useful isotopically labeled research compound.

Impurity Fluocinolone Acetonide EP Impurity A Applications Fluocinolone Acetonide-21-carboxylic Acid, is a derivative of Fluocinolone Acetonide (F455800), which is a Corticosteroid, used in dermatology to reduce skin inflammation and relieve itching References Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964), Emerson, M.V., et al.: BioDrugs, 21, 245 (2007),

Stability Hygroscopic Applications Dexamethasone 21-Phosphate Dimer is a derivative of Dexamethasone (D298800), a glucocorticoid used as an anti-inflammatory agent. Dexamethasone regulates T cell survival, growth, and differentiation. Dexamethasone 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)

Applications (5α)-Androst-3-en-17-one is a new potent steroidal aromatase inhibitor. Aromatase inhibitors are a class of drugs used in the treatment of breast cancer in postmenopausal women and gynecomastia in men References Varela, C. L., et al.: Bioorg. Med. Chem., 24, 2823 (2016), Dai, Y., et al.: Eur. J. Med. Chem., 45, 5612 (2010)

Glycoprotein hormones alpha chain Protein, Canine, Recombinant (His & Myc) is expressed in E. coli.

Applications The major human metabolite, a labelled bile acid which inhibits radioligand binding to muscarinic M1, but not to M2 or M3 receptors. References Javitt, N.B., et al.: J. Clin. Invest., 47, 1002 (1968), Bowmer, C., et al.: J. Pharm. Pharmacol., 37, 812 (1985), Ha, C., et al.: J. Biomed. Sci., 7, 114 (2000), Zaton, A., et al.: Chem. Biol. Interact., 124, 1 (2000),

Applications Isotope labelled Estrone (E889050), which is a metabolite of 17β-Estradiol (E888000). During the metabolism, it is in rapid equilibrium with Estriol (E888960) and 17β-Estradiol (E888000) (1). Causes the feminization of male fish at human and animal waste sites (2).Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA), environmental, and food contaminants. References 1. Both, D. et al.: Anal. Prof. Drug Subst. 1983 12 pp135-1892. Goodman-Gruen, D. et al.: J. Clin. Endocrinol. Metab. 1996 Aug;81(8):2999-3003.