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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Endocrinology & Hormones > EquolCAS：531-95-3
Molecular Formula：C15H14O3
Molecular Weight：242.27
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 531-95-3 |
| Name | Equol |
| Molecular Formula | C15H14O3 |
| Molecular Weight | 242.27 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 208-522-2 |
| MDL | MFCD00200962 |
| SMILES | OC1=CC=C2C[C@@H](C3=CC=C(O)C=C3)COC2=C1 |
| Target Point | Estrogen Receptor/ERR |
| Passage | Endocrinology & Hormones |
| Background | It is a high-affinity ligand for estrogen receptor beta. |
| Biological Activity | Equol是雌激素受体β的高亲和力配体。[1-3] |
| In Vitro | Equol显示对ERβ的最大亲和力(Ki = 0.73±0.2 nM)，而其对ERα的亲和力(Ki = 6.41±1 nM)相对较差[1]。Equol抑制LnCaP，DU145和PC3人前列腺癌细胞系的生长。Equol通过下调细胞周期蛋白B1和CDK1并上调CDK抑制剂(p21和p27)以及通过上调Fas配体(FasL)诱导细胞凋亡，导致PC3细胞G2 / M期细胞周期停滞。)和促凋亡Bim的表达。Equol增加FOXO3a的表达，降低p-FOXO3a的表达并增强FOXO3a的核稳定性。Equol还降低MDM2的表达，MDM2作为p-FOXO3a的E3泛素连接酶，从而阻止蛋白酶体对p-FOXO3a的降解[2]。 Equol可能通过激活PKA信号传导对映选择性地增加INS-1细胞的存活。Equol可能具有作为抗2型糖尿病药物的应用。在INS-1胰腺β细胞中，Equol诱导Ser133上cAMP反应元件结合蛋白的磷酸化，并诱导cAMP反应元件介导的转录[3]。 |
| In Vivo | Equol与第33天的对照相比，抑制肿瘤生长43.2％和28.4％，表明该化合物没有明显的毒性[2]。 |
| Cell Experiment | 将PC3细胞接种在96孔培养板(约5×103细胞/孔)中并在37℃下培养过夜。接下来，将细胞与含有指定浓度的Equol和/或DMSO的培养基在37℃下孵育72小时。通过MTT测定确定细胞活力[2]。 |
| Animal Experiment | 小鼠：将小鼠随机分成三组，每组六只小鼠，并通过胃内给药进行治疗。实验组用10mg / kg或20mg / kg体重的Equol处理(小鼠每天处理33天)。对照组用相同体积的0.01mL芝麻籽油和0.09mL生理盐水处理。每三天检查肿瘤大小[2]。 |
| Data Literature Source | [1]. 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. [2]. Lu Z， et al. S-equol， a Secondary Metabolite of Natural Anticancer Isoflavone Daidzein， Inhibits Prostate Cancer Growth In Vitro and In Vivo， Though Activating the Akt/FOXO3a Pathway. Curr Cancer Drug Targets. 2016; 16 (5) :455-65. [3]. Horiuchi H， et al. S-equol nantioselectively activates cAMP-protein kinase A signaling and reduces alloxan-induced cell death in INS-1 pancreatic β-cells. J Nutr Sci Vitaminol (Tokyo) . 2014; 60 (4) :291-6. |
| Unit | Bottle |
| Specification | 5mg 10mg 25mg |
是雌激素受体β (estrogen receptor β) 的高亲和力配体。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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