2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR Phosphodiesterase (PDE)
  4. EL244

EL244 是一种 Autotaxin (ATX) 抑制剂 (IC50 = 50 nM) 和 PPARγ 激动剂 (IC50 = 1.3 μM; Kd = 1.3 μM)。EL244 在人源 HepG2 细胞中显示出较低的细胞毒性 (EC50 = 81.2 μM)，且对心脏 hERG 钾离子通道的抑制作用极微 (12% at 25 μM)。在体内，EL244 能显著降低肺部溶血磷脂酸水平、减轻纤维化并恢复呼吸功能且全身吸收有限。EL244 可用于特发性肺纤维化研究。

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EL244

EL244 Chemical Structure

CAS No. : 3047548-70-6

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规格 价格 是否有货
1 mg ￥1600
询问价格 & 货期
5 mg ￥3978
询问价格 & 货期
10 mg 询价 询问价格 & 货期
25 mg 询价 询问价格 & 货期
50 mg 询价 询问价格 & 货期

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Customer Review

EL244 相关抗体

Top Publications Citing Use of Products

查看 PPAR 亚型特异性产品:

查看所有亚型
PPARα PPARβ/δ PPARγ PPAR PPARδ

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research[1].

IC50 & Target[1]

PPAR-γ

1.3 μM (IC50)

Autotaxin

50 nM (IC50)

体内研究
(In Vivo)

EL244 (15 mg/kg, 吸入给药) 在 Bleomycin (HY-108345) 诱导的肺纤维化小鼠模型中展现出良好的肺部靶向药代动力学特征，具体表现为肺部滞留性高、局部清除缓慢以及全身吸收有限[1]。
EL244 (15 mg/kg，吸入给药，每日一次，持续 15 天) 在 Bleomycin 诱导的肺纤维化小鼠模型中表现出抗纤维化的预防和缓解作用[1]。
EL244 (30 mg/kg，腹腔注射) 在 Bleomycin 诱导的肺纤维化小鼠模型中展现出良好的药代动力学特征：在 1 小时内达到 40 μM 的血浆浓度，并能在长达 3 小时内将浓度维持在约 35 μM，甚至在给药 9 小时后仍可以约 15 μM的浓度被检出，其最大药效学效应也恰好出现在 3 小时的时间点[1]。

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

Animal Model: BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
Dosage: 15 mg/Kg
Administration: Inhaled administration, once daily for 7 days
Result: Diminished inflammation, Appeared fibrotic regions.
Restored all assessed respiratory functions and reduced vascular permeability.
Demonstrated strong anti-fibrotic effects, significantly reducing soluble collagen in BALF and Col1a1 expression in lung tissue.
Reduced collagen deposition and fewer and smaller fibrotic regions.
Animal Model: BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
Dosage: 15 mg/Kg
Administration: Inhaled administration, once daily for 15 days
Result: Improved respiratory functions.
Reduced BLM-induced pulmonary oedema and inflammation.
Reduced Soluble collagen levels in BALF and Col1a1 mrna expression in lung tissue.
Attenuated collagen deposition and the reduction of fibrotic regions.
Not caused any appreciable toxicity in the liver, as indicated by the ALT/AST levels.
分子量

537.46

Formula

C25H26Cl2N2O5S
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

EL244 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

EL2443047548-70-6EL 244EL-244PPARPhosphodiesterase (PDE)Peroxisome proliferator-activated receptorsATXPPARγhuman HepG2 cellspotassium channelidiopathic pulmonary fibrosisInhibitorinhibitorinhibit

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目录号：
HY-179580
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