受注:045-509-1970 |
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Synonyms | GI198745, GG-745 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C27H30F6N2O2 |
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分子量 | 528.53 | CAS No. | 164656-23-9 | |
Solubility (25°C)* | 体外 | DMSO | 106 mg/mL (200.55 mM) | |
Ethanol | 25 mg/mL (47.3 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT). |
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in vitro | Dutasteride inhibits type-1 5AR and type-2 5AR with IC50 of 6 nM and 7 nM, respectively. Dutasteride is 60-fold more potent than Finasteride in its initial Ki versus type 1 5AR and ~5-fold more rapid in inactivating the enzyme. [1] Dutasteride inhibits (3)H-T conversion to (3)H-DHT and, as anticipated, inhibits T-induced secretion of PSA and proliferation in LNCaP cells. Dutasteride also inhibits DHT-induced PSA secretion and cell proliferation with IC50 of 1 μM in LNCaP cells. Dutasteride competes for binding the LNCaP cell AR with an IC50 of 1.5 μM. Dutasteride (10–50 μM) results in enhanced cell death, possibly by apoptosis, in steroid-free medium. [2] Dutasteride reduces cell viability and cell proliferation in androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer(PCa) cell lines. Dutasteride results in overexpressed genes included genes encoding for proteins involved in biosynthesis and metabolism of androgen (HSD17B1;HSD17B3;CYP11B2), androgen receptor and androgen receptor co-regulators (AR;CCND1), and signal transduction(ERBB2; V-CAM; SOS1) whereas, underexpressed genes (KLK3; KLK2; DHCR24) are androgen-regulated genes (ARGs) in androgen-responsive (LNCaP) cell. [3] Dutasteride inhibits FASN mRNA, protein expression and enzymatic activity in prostate cancer cells. [4] |
in vivo | Dutasteride (100 mg/kg/day) has prostates about half as large as those in intact male rats treated with vehicle alone. Dutasteride is orally bioavailable and because of its mechanism of action it easily overcomes the potential liability of being >99% plasma protein bound. [1] |
細胞アッセイ | 細胞株 | LNCaP Cells |
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濃度 | 1 μM | |
反応時間 | 5 days | |
実験の流れ | Cells were treated with various concentrations of drug for 5 days. |
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動物実験 | 動物モデル | Male Sprague-Dawley rats |
投薬量 | 0.5 mg/kg | |
投与方法 | i.g. gavage |
An integrated in vitro/in silico approach to assess the anti-androgenic potency of isobavachin [ Food Chem Toxicol, 2023, 176:113764] | PubMed: 37019376 |
Impact of short-term Dutasteride treatment on prostate-specific membrane antigen expression in a mouse xenograft model [ Cancer Rep (Hoboken), 2021, e1418] | PubMed: 34008909 |
Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12] | PubMed: 33232663 |
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction [ Drug Test Anal, 2020, 10.1002/dta.2917] | PubMed: 32852861 |
Concentration-dependent effects of dutasteride on prostate-specific membrane antigen (PSMA) expression and uptake of 177 Lu-PSMA-617 in LNCaP cells [ Prostate, 2019, 10.1002/pros.23868] | PubMed: 31233227 |
Inhibition of dihydrotestosterone synthesis in prostate cancer by combined frontdoor and backdoor pathway blockade. [ Oncotarget, 2018, 9(13):11227-11242] | PubMed: 29541409 |
Serum‐free complete medium, an alternative medium to mimic androgen deprivation in human prostate cancer cell line models [Fiandalo MV Prostate, 2018, 78(3):213-221] | PubMed: 29194687 |
Pharmacological upregulation of prostate‐specific membrane antigen (PSMA) expression in prostate cancer cells [Kranzbühler B Prostate, 2018, 78(10):758-765] | PubMed: 29633296 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。