Dutasteride-13C,15N,d
Dutasteride-13C,15N,d is 15N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
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- Formule: C2613CH29DF6N15NO2
- Masse moléculaire:531.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Dutasteride inhibits 3H-T conversion to 3H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC50 approximately 1 μM)[2]. Dutasteride competes for binding the LNCaP cell AR with an IC50 approximately 1.5 μM. High concentrations of dutasteride (10-50 μM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis[2]. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa)) [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 164656-23-9
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Masse moléculaire 531.52
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Formule C2613CH29DF6N15NO2
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SMILES
O=[13C]([C@H]1C([2H])C[C@]2([H])[C@]1(C)CC[C@]3([H])[C@@]4(C)C=CC([15NH][C@]4([H])CC[C@]32[H])=O)NC5=CC(C(F)(F)F)=CC=C5C(F)(F)F
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Synonyms
GG 745-13C,15N,d; GI 198745-13C,15N,d
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. Lazier CB, et al. Dutasteride, the dual 5alpha-reductase inhibitor, inhibits androgen action and promotes cell death in the LNCaP prostate cancer cell line. Prostate. 2004 Feb 1;58(2):130-44. [Content Brief]
[3]. Biancolella M, et al. Effects of dutasteride on the expression of genes related to androgen metabolism and related pathway in human prostate cancer cell lines. Invest New Drugs. 2007 Oct;25(5):491-7. [Content Brief]
[4]. Bramson HN, et al. Unique preclinical characteristics of GG745, a potent dual inhibitor of 5AR. J Pharmacol Exp Ther. 1997 Sep;282(3):1496-502. [Content Brief]
[5]. Andriole GL, et al. Clinical usefulness of serum prostate specific antigen for the detection of prostate cancer is preserved in men receiving the dual 5alpha-reductase inhibitor dutasteride. J Urol. 2006 May;175(5):1657-62. [Content Brief]
[6]. Margiotta-Casaluci L, et al. Mode of action of human pharmaceuticals in fish: the effects of the 5-alpha-reductase inhibitor, dutasteride, on reproduction as a case study. Aquat Toxicol. 2013 Mar 15;128-129:113-23. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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