2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. FXR PPAR
  4. dual FXR/PPARδ agonist-2

dual FXR/PPARδ agonist-2 是一种FXR/PPARδ 双重激动剂，通过 FXR 激动剂 GW-4064 与 PPARδ 激动剂 GW-0742 杂交产生。dual FXR/PPARδ agonist-2 具有强效的双靶点活性，其 FXR 激动作用的半数有效浓度 (EC50) 为 12.28 nM，在 100 nM 浓度下对 PPARδ 的激活率为 69%。dual FXR/PPARδ agonist-2 在肺纤维化小鼠模型中显示出抗纤维化作用。

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dual FXR/PPARδ agonist-2

dual FXR/PPARδ agonist-2 Chemical Structure

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dual FXR/PPARδ agonist-2 相关抗体

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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

dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model[1].

IC50 & Target[1]

FXR

12.28 nM (EC50)

体内研究
(In Vivo)

dual FXR/PPARδ agonist-2 (Compound 10g) (40 mg/kg，腹腔注射，每日一次，连续 21 天) 在博来霉素 (BLM) (HY-108345) 诱导的肺纤维化小鼠模型中，可显著减轻胶原蛋白沉积并降低 α-平滑肌肌动蛋白 (α-SMA) 的表达[1]。

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

Animal Model: Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice models[1]
Dosage: 40 mg/kg
Administration: Intraperitoneally injection, daily for 21 days
Result: Reduced lesion density (fewer and smaller foci) and diminished septal thickening.
Suppressed collagen accumulation and fibrotic progression.
Attenuated α-SMA deposition.
分子量

519.55

Formula

C26H29N7O5
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

dual FXR/PPARδ agonist-2 相关分类

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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:

dual FXR/PPARδ agonist-2FXRPPARNR1H4Peroxisome proliferator-activated receptorsPulmonary fibrosisBleomycinCollagenα-SMAInhibitorinhibitorinhibit

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