规格

价格

库存

数量

1 mg

¥ 397

现货

2 mg

¥ 595

现货

5 mg

¥ 997

现货

10 mg

¥ 1,560

现货

25 mg

¥ 2,790

现货

50 mg

¥ 4,150

现货

100 mg

¥ 5,920

现货

1 mL x 10 mM (in DMSO)

¥ 1,090

现货

生物活性

产品描述	GSK5182 is a specific inverse agonist of estrogen-related receptor γ (ERRγ), an orphan nuclear receptor involved in metabolism and cellular homeostasis. The compound inhibits ERRγ transcriptional activity while paradoxically increasing its protein stability, blocking ubiquitination and degradation mediated by the E3 ligase Parkin. In cellular models, GSK5182 suppresses RANKL-induced osteoclast differentiation by over 50% at low micromolar concentrations and accelerates osteoclast apoptosis via caspase-3 activation. Researchers use GSK5182 to study ERRγ function in bone metabolism, osteoarthritis pathogenesis, and radioiodine sensitivity in thyroid cancer cells, where it enhances sodium-iodide symporter activity through MAP kinase signaling.
靶点活性 (IC₅₀)	ERRγ:79 nM
体外活性	Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5^[1].
体内活性	a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production^[2].
细胞实验	Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours

化学信息

分子量	417.5399
分子式	C₂₇H₃₁NO₃
CAS No.	877387-37-6
Smiles	CN(C)CCOC1=CC=C(C=C1)C(=C(CCCO)C1=CC=CC=C1)C1=CC=C(O)C=C1
密度	1.132 g/cm3 (Predicted)

储存&溶解度

存储

Keep away from direct sunlight,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 80.00 mg/mL (191.60 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Saline: < 8 mg/mL (19.16 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+ 5% Tween 80 + 45% Saline: 8.00 mg/mL (19.16 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3950 mL	11.9749 mL	23.9498 mL	119.7490 mL
5 mM	0.4790 mL	2.3950 mL	4.7900 mL	23.9498 mL
10 mM	0.2395 mL	1.1975 mL	2.3950 mL	11.9749 mL
20 mM	0.1197 mL	0.5987 mL	1.1975 mL	5.9875 mL
50 mM	0.0479 mL	0.2395 mL	0.4790 mL	2.3950 mL
100 mM	0.0239 mL	0.1197 mL	0.2395 mL	1.1975 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

GSK5182

GSK5182

产品介绍

引用文献

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剂量转换

关键词

GSK5182

GSK5182

GSK5182 相关产品

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