2. Metabolic Enzyme/Protease Anti-infection
  3. UGT Bacterial
  4. 16-Epiestriol

16-Epiestriol  (Synonyms: 16-epi-Estriol; 16β,17β-Estriol)

目录号: HY-130046
一键复制产品信息 纯度: 99.04%
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16-Epiestriol 是雌三醇的一种天然立体异构体及抗炎剂，靶向 UGT。16-Epiestriol 对人 UGT1A10 和 UGT2B7 的 Ki 分别为 98.1 μM 和 162 μM。16-Epiestriol 作为葡萄糖醛酸化底物，3-OH、16-OH 和 17-OH 位点可被多种 UGT 酶修饰，且在肝微粒体中主要发生于 16-OH 和 17-OH 位点，而在肠微粒体中三个位点均可发生反应。16-Epiestriol 通过阻断前列腺素和白细胞浸润介导的水肿来作用于 II 期炎症过程。且 16-Epiestriol 不具备糖原生成活性或影响血糖水平，是炎症性疾病研究中的重要候选分子。

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16-Epiestriol

16-Epiestriol Chemical Structure

CAS No. : 547-81-9

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2.5 mg ￥980
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Other Forms of 16-Epiestriol:

16-Epiestriol 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

16-Epiestriol is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases[1][2].

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

16-Epiestriol (200 μM; 15-60 min) 可被重组人源 UGT1A1、UGT1A7、UGT1A8、UGT2B15、UGT1A3、UGT2A1、UGT2B4 和 UGT2B17 靶向，这些酶对其表现出低水平的葡糖醛酸化活性，且对 3-OH 或 16-OH 具有区域选择性[1]。
16-Epiestriol (0.2-300 μM; 15-60 min) 会被混合人肠微粒体靶向，后者优先催化其 3-OH 位的葡萄糖醛酸化，对应的 Vmax 为 4111 pmol/min/mg、Km 为 50 ± 3 μM，同时在 16-OH 和 17-OH 位具有次级活性[1]。
16-Epiestriol (200 μM, 0.2-300 μM; 15-60 min) 可被重组人源 UGT2B7 靶向，该酶催化其 16-OH 葡萄糖醛酸化反应，对应的 Vmax 为 3866 pmol/min/mg，Km 为 38.4 μM，且存在底物抑制作用，Ki 为 162 μM[1]。
16-Epiestriol (0.2-300 μM; 15-60 min) 可被重组人源 UGT1A10-F93G 靶向，该酶催化其 3-OH 位点的葡萄糖醛酸化反应，对应的 Vmax 为 2249 pmol/min/mg，Km 为 186 μM，与野生型 UGT1A10 相比表现出更低的周转效率和更高的 Km[1]。
16-Epiestriol (0.2-300 μM; 15-60 min) 会被混合人肝微粒体靶向作用，后者优先催化其 16-OH 葡萄糖醛酸化，对应的 Vmax 为 8011 pmol/min/mg，Km 为 33 μM，而在 3-OH 和 17-OH 位点的活性则低得多[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

16-Epiestriol 相关抗体:
体内研究
(In Vivo)

16-Epiestriol (10-20 mg/kg; i.p.) 在大鼠中表现出强效抗炎活性，其中 20 mg/kg 剂量在 5 小时时可将角叉菜胶诱导的足肿胀减轻 58%，且其等摩尔效力是 Hydrocortisone (HY-N0583) 的两倍以上[2]。
16-Epiestriol (60 μg/rat; s.c.; 在第 0, 2, 4, 和 6 h 时注射) 在去肾上腺大鼠中未表现出显著的糖原生成活性，因为与未处理对照组相比，它不会改变血浆或肝脏葡萄糖浓度[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, mean body weight ~200 g)[2]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose
Result: Reduced paw volume change to 0.22 mL (±0.05 SEM) at 1 h, 0.59 mL (±0.05 SEM) at 2 h, 0.71 mL (±0.05 SEM) at 3 h, and 0.50 mL (±0.06 SEM) at 5 h at 10 mg/kg.
Reduced paw volume change to 0.17 mL (±0.03 SEM) at 1 h, 0.44 mL (±0.05 SEM) at 2 h, 0.65 mL (±0.04 SEM) at 3 h, and 0.48 mL (±0.05 SEM) at 5 h at 20 mg/kg.
Reduced edema by 58% at 5 h compared to untreated controls at 20 mg/kg.
Reduced edema by 56% at 5 h on an equimolar basis, which is more than twice the efficacy of hydrocortisone.
Showed statistically significantly less edema at 5 h compared to untreated and hydrocortisone-treated groups (p < 0.001 by Student’s t-test) at 20 mg/kg.
Animal Model: Sprague-Dawley (adrenalectomized male, average body weight 185 g)[2]
Dosage: 60 μg/rat per dose; total cumulative dose 240 μg/rat (0.832 μmol/rat)
Administration: s.c.; four doses at 0, 2, 4, and 6 h
Result: Resulted in median plasma glucose concentration of 79.0 mg/dL and median liver glucose concentration of 93.9 μg/g of liver.
Showed no statistically significant differences in median plasma or liver glucose concentrations relative to untreated control groups.
分子量

288.38

Formula

C18H24O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

雌三醇EP杂质F
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 99.04%

COA (286 KB)

产品使用指南 (1538 KB)
参考文献

16-Epiestriol 相关分类

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Keywords:

16-Epiestriol547-81-916-epi-Estriol 16β,17β-Estriol雌三醇EP杂质FUGTBacterialUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseUGT2B17UGT1A10UGT2B7UGT1A7UGT1A3UGT1A8UGT1A1UGT2B4UGT2A1UGT2B15Inhibitorinhibitorinhibit

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