2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. Gala-SR

Gala-SR (Gala-SR1078) 是一种 RORα 激动剂。Gala-SR 通过增强昼夜节律的振幅来改善节律紊乱。Gala-SR 可用于牙周炎的研究。

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Gala-SR

Gala-SR Chemical Structure

CAS No. : 3092129-97-7

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Gala-SR 相关抗体

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RORγ RORα RORβ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gala-SR (Gala-SR1078) is an RORα agonist. Gala-SR ameliorates rhythm disorders by enhancing the amplitude of the circadian rhythm. Gala-SR can be used for the study of periodontitis[1].

IC50 & Target

RORα

 

体外研究
(In Vitro)

Gala-SR (1-100 μM，24-72 小时) 通过半乳糖修饰显著改善了其与人 U2OS 细胞的相容性[1]。
Gala-SR (5 μM，24 小时) 显著上调 HepG2 细胞中 RORα/γ 的直接靶基因 G6Pase 和 FGF21 的 mRNA 表达[1]。
Gala-SR (5 μM) 选择性地增强 HEK293T 细胞中 RORα 的转录激活活性[1]。
敲低 RORα 后，Gala-SR (5 μM，24 小时) 对 G6Pase 和 FGF21 基因的激活作用显著降低[1]。
Gala-SR (5 μM) 主要通过其可水解的半乳糖修饰靶向并激活 RORα[1]。
Gala-SR (2-5 μM) 显著增强了 U2OS 细胞中 BMAL1 和 Per2 报告基因的生物发光水平和节律振幅，并增强了 BMAL1 蛋白的表达[1]。

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

Gala-SR 相关抗体:

Real Time qPCR[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Upregulated the mRNA expression of G6Pase and FGF21, direct target genes of RORα/γ, in HepG2 cells.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice 10 mg/kg i.p. T1/2 3.43 h
Mice 10 mg/kg i.v. T1/2 2.49 h
Mice 10 mg/kg i.p. Tmax 0.5 h
Mice 10 mg/kg i.v. Tmax 0.5 h
Mice 10 mg/kg i.p. Cmax 1313.1 ng/mL
Mice 10 mg/kg i.v. Cmax 4992.46 ng/mL
Mice 10 mg/kg i.p. AUC 6077.31 ng·h/mL
Mice 10 mg/kg i.v. AUC 8176.18 ng·h/mL
Mice 10 mg/kg i.p. MRTINF_obs 4.5 h
Mice 10 mg/kg i.v. MRTINF_obs 2.97 h
体内研究
(In Vivo)

Gala-SR (10 mg/kg，关灯前 1 小时腹腔注射，每日一次，持续 2 周) 可显著增强小鼠的活动节律振幅和总活动量[1]。
Gala-SR (10 mg/kg，开灯时，一次) 可增强 PER2::LUC 敲入小鼠的肝脏荧光素酶信号传导，表明 BMAL1 表达增强[1]。
Gala-SR (10 mg/kg，腹腔注射，每日一次，持续 3 周) 可恢复牙周炎小鼠的牙周组织节律振幅，抑制 NF-κB 炎症通路，并减轻牙周炎相关的骨丢失[1]。

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

Animal Model: C57BL/6J mice were first acclimatized to a 12-hour light/12-hour dark (L:D) condition for 2 weeks, and then switched to continuous darkness (D:D) to induce circadian rhythm disorder[1].
Dosage: 10 mg/kg
Administration: 1 hour before the end of the light exposure, i.p., once daily for 2 weeks
Result: Significantly enhanced the amplitude of the activity rhythm and the total activity level in mice.
Animal Model: PER2::LUC gene knock-in mice[1].
Dosage: 10 mg/kg
Administration: I.p., once, light start time
Result: Enhanced liver luciferase signaling indicates increased BMAL1 expression.
Animal Model: Male C57BL/6 mice, 2 months old, were housed under disrupted conditions for 4 weeks, and a ligature was placed around the cervix of the maxillary second molar to establish the murine periodontitis model[1].
Dosage: 10 mg/kg
Administration: I.p., once daily for 3 weeks
Result: Significantly reduced alveolar bone resorption (increased bone volume/total volume, reduced bone resorption height).
Reduced inflammatory cell infiltration and osteoclast activity.
Downregulated pro-inflammatory factors (TNF-α, IL-6) and upregulates anti-inflammatory factors (IL-10).
分子量

623.42

Formula

C24H22F9NO8
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Gala-SR 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gala-SR3092129-97-7Gala-SR1078RORRAR-related orphan receptorCircadian rhythmRORα agonistBone lossPeriodontitisInhibitorinhibitorinhibit

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目录号：
HY-179514
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