Spironolactone

製品コードS4054 バッチS405402

印刷

化学情報

Chemical Structure 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 20 mg/mL (48.01 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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] This compound 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 this compound (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
The stable MR, MRS810L, 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

  • http://www.ncbi.nlm.nih.gov/pubmed/?term=20650892
  • http://www.ncbi.nlm.nih.gov/pubmed/?term=4376096

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：

Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14] PubMed: 40185092
The macrophage-intrinsic MDA5/IRF5 axis drives HIV-1 intron-containing RNA-induced inflammatory responses [ J Clin Invest, 2025, 135(16)e187663] PubMed: 40493408
Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs [ Biomed Pharmacother, 2024, 180:117523] PubMed: 39405910
Profiling of ERBB receptors and downstream pathways reveals selectivity and hidden properties of ERBB4 antagonists [ iScience, 2024, 27(2):108839] PubMed: 38303712
Glucocorticoids Selectively Inhibit Hippocampal CA1 Pyramidal Neurons Activity Through HCN Channels [ Int J Mol Sci, 2024, 25(22)11971] PubMed: 39596039
Pannexin 1 and pannexin 3 differentially regulate the cancer cell properties of cutaneous squamous cell carcinoma [ J Physiol, 2024, 10.1113/JP286172] PubMed: 39560179
An Integrated Approach of Bioassays and Non-Target Screening for the Assessment of Endocrine-Disrupting Activities in Tap Water and Identification of Novel Endocrine-Disrupting Chemicals [ Toxics, 2024, 12(4)247] PubMed: 38668470
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

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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