| 生物活性 |
4,4'-Sulfonyldiphenol, a substitute for Bisphenol A , is widely used in industrial and consumer products. 4,4'-Sulfonyldiphenol is an oally ative estrogen receptor (ER) agonist and can competitively bind to thyroid hormone receptors (TR) with IC50 values for TRα and TRβ are 2650 μM and 2294 μM respectively, thereby affecting breast development and reducing the expression of androgen receptor (AR) in fetal testes. 4,4'-Sulfonyldiphenol promotes the progression of glioblastoma by upregulating the EZH2 mediated PI3K/AKT/mTOR pathway. Under chronic exposure, 4,4'-Sulfonyldiphenol can cause significant lipid deposition and dyslipidemia in the mouse liver by upregulating JunB and Atf3, and has a role in causing obesity at low doses. 4,4'-Sulfonyldiphenol induces intestinal inflammation by altering the intestinal microbiome. 4,4'-Sulfonyldiphenol accelerates the progression of atherosclerosis in zebrafish embryo larvae。
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| 体外研究 |
4,4 '- Sulfonyldiphenyl (0-50 μM) can induce thyroid hormone (TH) - dependent proliferation of GH3 cells and inhibit T3 induction in the presence of T3 .
4,4 '- Sulfonyldiphenyl (100 μM, 24 hours) significantly increased lipid deposition in AML12 and primary liver cells via the JunB/ATF3 axis.
4,4 '- Sulfonyldiphenyl (0.001-100 μM, 4-24 hours) promotes proliferation and migration of U-87 MG cells at a concentration of 0.1 µM, and appears to be involved in the EZH2 mediated activation of PI3K/AKT/mTOR pathway .
4,4 '- Sulfonyldiphenol (0.01-1 μM, 0-24 hours) can enhance the formation of oxidized low-density lipoprotein (oxLDL) foam cells in macrophages.
Cell Proliferation Assay
| Cell Line: |
U-87 MG cells |
| Concentration: |
0, 0.001, 0.01, 0.1, 1, 10 and 100 μM |
| Incubation Time: |
4 and 8 hours |
| Result: |
Significantly increased the proliferation rate at 0.1 μM, and the effect was more significant after 8 hours of treatment than after 4 hours. |
Cell Migration Assay
| Cell Line: |
U-87 MG cells |
| Concentration: |
0.1 μM |
| Incubation Time: |
0, 2, 4, 6, 8, 10 and 12 hours |
| Result: |
Significantly increased the mobility within 12 hours. |
Cell Invasion Assay
| Cell Line: |
U-87 MG cells |
| Concentration: |
0.1, 1 and 10 μM |
| Incubation Time: |
24 hours |
| Result: |
Induced glioblastoma invasion in U-87 MG cells. |
CRT-PCR
| Cell Line: |
U-87 MG cells |
| Concentration: |
0.1 μM |
| Incubation Time: |
4 and 8 hours |
| Result: |
Increased the mRNA level of EZH2. |
Western Blot Analysis
| Cell Line: |
U-87 MG cells |
| Concentration: |
0.1 μM |
| Incubation Time: |
4 and 8 hours |
| Result: |
Increased the expression of EZH2, p-PI3K, p-AKT, p-mTOR and p-4E-BP1.
Decreased the expression of PIK3IP1. |
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| 体内研究 |
4,4 '- Sulfonyldiphenyl (2-2000 μg/kg, orally, from day 9 of pregnancy until day 2 or 20 of lactation) alters the growth of breast epithelium and makes male mice more sensitive to additional estrogen exposure during puberty.
4,4 '- Sulfonyldiphenyl (0.2-50 μg/kg, orally, once daily from day 0 of pregnancy until offspring reach 23 weeks of age) can lead to obesity in male mice at low doses, as well as after perinatal and chronic exposure.
4,4 '- Sulfonyldiphenyl (0-10 μM, single dose) can induce TH responsive gene transcription in black spotted lateral fold tadpoles, but changes T3 induced gene transcription in a biphasic concentration response at T3.
4,4 '- Sulfonyldiphenol (0.1-1 mg/kg, gavage, once daily, for 3 months) induced significant lipid deposition and dyslipidemia in the liver of mice, and increased susceptibility to metabolic dysfunction associated fatty liver disease (MASLD).
4,4 '- Sulfonyldiphenol (0.1-1 mg/kg, gavage, once daily, for 3 months) induces intestinal inflammation by altering the gut microbiota of mice.
4,4 '- Sulfonyldiphenol (0-100 μg/L, lasting for 15-45 days) accelerated the progression of atherosclerotic cardiovascular disease (ASCVD) in zebrafish embryonic larva model.
| Animal Model: |
Long-term and short-term exposure effect assessment established in female CD-1 mice |
| Dosage: |
2 and 200 μg/kg (long-term); 2, 200, and 2000 μg/kg (short-term) |
| Administration: |
Oral administration (p.o.), once daily starting on pregnancy day 9 through lactation day 20 (long-term) and starting on pregnancy day 9 through lactation day 2 (short-term) |
| Result: |
Showed signs of ductal formation in the mammary gland and significantly enlarged the intercellular spaces between the tissues.
Increased ERα expression in epithelial cells and dose-dependently decreased AR expression in the stroma.
Increased the right duct area in all groups, and the left duct area also increased significantly in the high-dose group.
Altered the response of male mice to a pre-pubertal estrogen challenge. |
| Animal Model: |
High fat diet model established in pregnant C57Bl/6J mice |
| Dosage: |
0.2, 1.5, 50 µg/kg |
| Administration: |
Oral administration (p.o.) with water, once daily beginning at gestational day 0 and continuing in offspring up to 23-weeks old |
| Result: |
Significantly increased in body weight and fat mass on a high-fat diet.
Had no effect on the food intake and energy expenditure.
Exhibited a weak but significant hypercholesterolemia with a fold increase of 1.21 and 1.29 at 1.5 and 50 µg/kg, respectively.
Showed a significant decrease of the AUC (increase of blood TG clearance).
Significantly increased the calculated HOMA-IR index in mice exposed to 1.5 and 50 µg/kg.
Induced a significant overexpression of SOCS3 mRNA and a significant mRNA down-regulation of INSR and adiponectin.
Induced a weak but significant decrease in mRNA expression of HSL and PPARγ genes in adipose tissue of male mice fed with a HFD. |
| Animal Model: |
MASLD model established in 7-week-old C57BL/6 male mice |
| Dosage: |
0.1 and 1 mg/kg |
| Administration: |
Oral gavage (i.g.), once daily for 3 months |
| Result: |
Induced MASLD phenotype: elevated LDL, increased NEFA, and elevated ALT.
Showed obvious lipid droplet accumulation. |
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| 分子式 |
C12H10O4S
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| 分子量 |
250.28
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| CAS号 |
80-09-1
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| 中文名称 |
4,4-二羟基二苯砜
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
2-8°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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| 溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (399.55 mM; Need ultrasonic)
配制储备液
| 浓度 溶剂体积 质量 |
1 mg |
5 mg |
10 mg |
| 1 mM |
3.9955 mL |
19.9776 mL |
39.9552 mL |
| 5 mM |
0.7991 mL |
3.9955 mL |
7.9911 mL |
| 10 mM |
0.3996 mL |
1.9978 mL |
3.9955 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
-
1.
请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80 → 45% saline
Solubility: ≥ 2.5 mg/mL (9.99 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.99 mM,饱和度未知) 的澄清溶液。
以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。
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2.
请依序添加每种溶剂: 10% DMSO → 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (9.99 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (9.99 mM,饱和度未知) 的澄清溶液。
以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中,混合均匀。
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