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Equol

カタログ番号GC16292

エクオールはエクオールのラセミ体です。

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Equol 化学構造

Cas No.: 94105-90-5

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$35.00
在庫あり
5mg
$30.00
在庫あり
25mg
$88.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of Equol

IC50: Not available.

Equol is an isoflavan produced by intestinal bacteria in response to soy isoflavone intake in human. It shows a wide range of activities including antioxidant activity, anti-inflammation activity and anticancer activity. It is reported that Equol specifically binds to 5α-DHT and has a modest affinity for recombinant estrogen receptor ERβ, which may be responsible for most of Equol’s biological properties. [1]

In vitro: In vitro studies were conducted to measure both the binding affinity of Equol for 5alpha-dihydrotestosterone (5alpha-DHT) and the effects of Equol treatment in human prostate cancer (LNCap) cells. It was found that Equol bound to 5alpha-DHT with maximum and half maxim concentrations of 100 nM and 4.8 nM, respectively. In addition, Equol significantly offset the increases in PSA levels from LNCap cells. [1]

In vivo: An in vivo study was performed to investigate effects of equol on rat prostate weight and circulating levels of sex steroid hormones. 1.0 mg/kg of Equol was injected to Long-Evans rats fed with a low isoflavone diet for 25 days. Findings from this study suggested that Equol significantly decreased rat prostate weights and down-regulated serum levels of 5alpha-DHT. However, this agent did not alter levels of LH, testosterone and estradiol. [1]

Clinical trials: A clinical study on hypercholesterolemic patients demonstrated that, after 4 weeks’ dietary intervention with a soy isoflavone-containing food, brachial artery-mediated vasodilatation in equol-producers was notably higher when compared with that in equol-nonproducers. Similar differential effects between equol-producers and nonproducers were aslo reported in arterial stiffness from a study on postmenopausal women taking tibolone. [2]

References:
[1]Lund TD, Blake C, Bu L, Hamaker AN, Lephart ED.  iEquol an isoflavonoid: potential for improved prostate health, in vitro and in vivo evidence. Reprod Biol Endocrin. 2011; 9(4): doi: 10.1186/1477-7827-9-4.
[2]Setchell DR and Clerici C.  Equol: Pharmacokinetics and biological actions. J Nutr. 2010 Jul; 140(7): 1363S–8S.

Protocol of Equol

Cell experiment:

Primary rat osteoblasts are treated with 0.01-1 μM equol, 0.01-1 μM E2 , or 0.01-1 μM equol/E2 combined with 1 μM ICI182780 for 24 or 48 hours. Then 10 mL 5 mg/mL MTT solution is added to each well. The plates are incubated at 37°C for 4 h, and then the supernatant is discarded and 100 mL DMSO is added to each well and mixed thoroughly before taking measurements in a microplate reader[3].

Animal experiment:

Rats: Equol or furosemide is administered orally at doses of 16, 40, and 100 mg/kg (in a volume of 16 mL/kg 5% arabic syrup) to groups of 3-9 rats (rats of a control group are administered vehicle only). Urine samples are collected for 6 h. Urinary sodium and potassium contents are measured by flame photometry[3]. Mouse: Equol is dissolved in water and administered orally to rats at a dose of 5 and 25 mg/kg BW for 8 weeks after a single dose of DMBA (100 mg/kg). As controls, rats are divided into vehicle alone and DMBA alone groups. In the second part, ICR mice are orally administered equol daily at a dose of 5 and 25 mg/kg BW for 7 weeks before a single dose of DMBA (34 mg/kg/week). After equol administration animals are followed for 1 week continuously. The control groups are the same as above and each group are comprised of six mice. Mice livers and mammary gland tumors are isolated, blotted, weighed, frozen in liquid nitrogen and stored at -70°C until assayed[5].

References:

[1]. Axelson M, et al. The identification of the weak oestrogen equol [7-hydroxy-3-(4'-hydroxyphenyl)chroman] in human urine. Biochem J. 1982 Feb 1;201(2):353-7.
[2]. Setchell KD, et al. S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9. human intestinal bacterial flora.
[3]. Wang J, et al. Equol promotes rat osteoblast proliferation and differentiation through activating estrogen receptor. Genet Mol Res. 2014 Jul 4;13(3):5055-63.
[4]. Gimenez I,et al. Renal and vascular actions of equol in the rat. J Hypertens. 1997 Nov;15(11):1303-8.
[5]. Choi EJ, et al. Anticancer mechanism of equol in 7,12-dimethylbenz(a)anthracene-treated animals. Int J Oncol. 2011 Sep;39(3):747-54.

Chemical Properties of Equol

Cas No. 94105-90-5 SDF
Chemical Name (3S)-3-(4-hydroxyphenyl)-3,4-dihydro-2H-chromen-7-ol
Canonical SMILES C1C(COC2=C1C=CC(=C2)O)C3=CC=C(C=C3)O
Formula C15H14O3 M.Wt 242.27
溶解度 ≥ 12.1mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Equol

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 4.1276 mL 20.6381 mL 41.2763 mL
5 mM 0.8255 mL 4.1276 mL 8.2553 mL
10 mM 0.4128 mL 2.0638 mL 4.1276 mL
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計算

In vivo Formulation Calculator (Clear solution) of Equol

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 16 reference(s) in Google Scholar.)

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