Spironolactone

製品コードS4054 バッチS405403

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₃₂O₄S
	分子量	416.57	CAS No.	52-01-7
Solubility (25°C)*	体外	DMSO	83 mg/mL (199.24 mM)
		Ethanol	27 mg/mL (64.81 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	Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.
in vitro	Spironolactone is a strong AR antagonist (IC50 ~ 77 nM), a weak GR antagonist (IC50 ~ 2.4 μM), and a weak PR agonist (EC50 ~ 740 nM). ^[1] Spironolactone inhibits androstanolone binding in rat prostate nuclei and androstanolone specific binding in rat prostate cytosol. ^[2]
in vivo	Spironolactone (1 mg/day) exerts anti-androgenic activity in rats. A single pretreatment of spironolactone (1 mg/rat) inhibits specific and saturable uptake of hormone into prostate induced by tracer dose administration of [³H]testosterone. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Transactivation Assays
キナーゼアッセイ	The stable MR, MR_S810L, GR, AR, and PR cell lines are cultured at 37℃ and 5% CO2 in DMEM/Ham’s F-12 medium with GlutaMAX supplemented with 10% (v/v) inactivated fetal calf serum, 20 mM HEPES, 1.4 mM sodium pyruvate, 1.8 mM sodium bicarbonate, and 1 mg/ml Geneticin. Subconfluent cultures are passaged using Accutase. All of the cell culture reagents are obtained from Invitrogen. The cells are seeded 24 h before testing in Optimem medium containing 2.5% FCS (v/v), 2mM glutamine, and 10 mM HEPES in 96- or 384-well plates. On the test day compounds are given in eight dilutions to the cells followed by the relevant EC50 concentration of each agonist. After an incubation time of 5–6 h, luciferase activity is determined using a luminescence detecting video camera system. The GraphPad Prism software is used for curve fitting and calculation of the IC50 and EC50 values. The IC50 and EC50 values from the luciferase assay are determined in at least three independent experiments performed in duplicate.
動物実験	動物モデル	Rats
	投薬量	0-1 mg/day
	投与方法	i.p.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , Leukemia, 2018, 32(1):111-119]

: Data from [Data independently produced by , , Antiviral Res, 2017, 146:76-85]

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：

LP-284, a small molecule acylfulvene, exerts potent antitumor activity in preclinical non-Hodgkin's lymphoma models and in cells deficient in DNA damage repair [ Oncotarget, 2023, 14:597-611]	PubMed: 37306526
NR3C2 inhibits the proliferation of colorectal cancer via regulating glucose metabolism and phosphorylating AMPK [ J Cell Mol Med, 2023, 27(8):1069-1082]	PubMed: 36950803
Direct actions of dapagliflozin and interactions with LCZ696 and spironolactone on cardiac fibroblasts of patients with heart failure and reduced ejection fraction [ ESC Heart Fail, 2022, 10.1002/ehf2.14186]	PubMed: 36303443
Inhibitors of Nucleotide Excision Repair Decrease UVB-Induced Mutagenesis-An In Vitro Study [ Int J Mol Sci, 2021, 22(4)1638]	PubMed: 33562002
Pannexin 1 binds β-catenin to modulate melanoma cell growth and metabolism [ J Biol Chem, 2021, S0021-9258(21)00252-0]	PubMed: 33647315
In vitro Assessment of Corticosteroid Effects of Eight Chiral Herbicides [ J Environ Sci Health B, 2020, 55(2):91-102]	PubMed: 31524045
Nucleotide excision repair is a potential therapeutic target in multiple myeloma [Szalat R, et al. Leukemia, 2018, 32(1):111-119]	PubMed: 28588253
Potential endocrine-disrupting effects of metals via interference with glucocorticoid and mineralocorticoid receptors. [ Environ Pollut, 2018, 242(Pt A):12-18]	PubMed: 29957541
Determination of endocrine-disrupting potencies of agricultural soils in China via a battery of steroid receptor bioassays [Zhang J, et al. Environ Pollut, 2018, 234:846-854]	PubMed: 29248852
Novel Pathways of Endocrine Disruption Through Pesticides Interference With Human Mineralocorticoid Receptors. [ Toxicol Sci, 2018, 162(1):53-63]	PubMed: 29149346

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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