Dutasteride

製品コードS1202 バッチS120202

化学情報

	Synonyms	GI198745, GG-745	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₇H₃₀F₆N₂O₂
	分子量	528.53	CAS No.	164656-23-9
Solubility (25°C)*	体外	DMSO	100 mg/mL (189.2 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).
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]

製品説明

Dutasteride (GI198745, GG-745) is a dual 5-α reductase inhibitor that inhibits conversion of testosterone to dihydrotestosterone (DHT).

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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	LNCaP Cells
	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.
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

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。

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