2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. ROR PPAR LXR
  4. SR-1903

SR-1903 是一种 RORγ、PPARγ 反向激动剂 (RORγ 和 PPARγ 的 IC50 分别为∼100 nM 和 209 nM) 和 LXR 激动剂 (EC50 为 154 nM)。SR-1903 在胶原诱导性关节炎和饮食诱导性肥胖小鼠模型中发挥抗炎和抗糖尿病功效。

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SR-1903 Chemical Structure

SR-1903 Chemical Structure

CAS No. : 1414248-06-8

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SR-1903 相关抗体

Top Publications Citing Use of Products

查看 ROR 亚型特异性产品:

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RORγ RORα RORβ

查看 PPAR 亚型特异性产品:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models[1].

IC50 & Target[1]

RORγ

~100 nM (IC50)

PPARγ

209 nM (IC50)

体外研究
(In Vitro)

SR1903 (10 μM) 减弱巨噬细胞中的 LPS (HY-D1056) 信号，抑制 TREM-1 基因表达[1]。
SR1903 增加巨噬细胞 RAW264.7 中 LXR 靶基因表达，包括参与巨噬细胞胆固醇流出基因 (ABCG1和SCD) 和脂质代谢基因 (ACACA 和 FASN)[1]。

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

SR-1903 相关抗体:
体内研究
(In Vivo)

SR1903 (20 mg/kg，腹腔注射，一天两次，共 16 天) 在胶原诱发性关节炎 (CIA) 小鼠中改善关节炎症状，防止胸腺细胞的丢失[1]。
SR1903 (20 mg/kg，腹腔注射，14 天) 改善饮食诱发性肥胖 (DIO) 小鼠代谢参数，并对肥胖相关的胸腺退化发挥保护作用[1]。

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

Animal Model: Collagen-induced arthritis (female DBA/1J mice were injected with chicken type II collagen on day 1, and then each animal received a boost injection of collagen on day 21)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), twice-a-day for a total of 16 days
Result: Demonstrated a reduction in arthritis clinic score at the conclusion of the study (day 34).
Did not cause enlargement of the liver.
Had enhanced thymocyte differentiation and survival compared to mice treated with either the selective LXR agonist GW3965 or the dual LXR agonist/RORγ inverse agonist T0901317.
Animal Model: Diet-induced obese (DIO) mouse (Male, 22 weeks of age, fed a high fat diet (60% kCal % fat))[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (i.p.), 14 days
Result: Improved fasting glucose levels and reduced total cholesterol and low density lipoprotein (LDL).
Improved both fasting and fed insulin levels.
Showed 15% weight loss and 17% reduction in fat mass after 14 days.
Reduced food intake.
Reduced leptin resistance and repressed Socs3 (suppressor of cytokine signaling-3) expression.
分子量

523.51

Formula

C27H27F6N3O
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

SR-1903 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

SR-19031414248-06-8SR1903SR 1903RORPPARLXRRAR-related orphan receptorPeroxisome proliferator-activated receptorsLiver X receptorAnti-inflammatoryArthritisObesityAntidiabeticRAW264.7DBA/1JDIO.Inhibitorinhibitorinhibit

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