2. GPCR/G Protein Apoptosis Metabolic Enzyme/Protease
  3. Adenosine Receptor Apoptosis PGC-1α
  4. LJ-2698

LJ-2698 是一种具有口服活性的腺苷 A3 受体 (Adenosine A3 Receptor) 拮抗剂。LJ-2698 可诱导巨噬细胞中抗炎细胞因子水平升高，还能显著增加肺部抗炎性 M2 型巨噬细胞数量。LJ-2698 可阻止小鼠肺泡腔扩大，恢复小鼠肺功能，抑制小鼠肺组织中的基质金属蛋白酶活性与肺细胞凋亡 (apoptosis)。LJ-2698 可预防糖尿病肾病小鼠的肾损伤，抑制小鼠的肾脂质蓄积，并提高肾组织中的 PGC1α 水平。LJ-2698 可用于肺气肿和糖尿病肾病的研究。

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LJ-2698

LJ-2698 Chemical Structure

CAS No. : 945457-84-1

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LJ-2698 相关抗体

Top Publications Citing Use of Products

查看 Adenosine Receptor 亚型特异性产品:

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LJ-2698 is an orally active adenosine A3 receptor antagonist. LJ-2698 induces increased levels of anti-inflammatory cytokines in macrophages and significantly elevates the number of anti-inflammatory M2 macrophages in the lung. LJ-2698 prevents alveolar cavity enlargement, restores pulmonary function, inhibits matrix metalloproteinase activity and pulmonary cell apoptosis in the lung tissues of mice. LJ-2698 prevents renal injury, inhibits renal lipid accumulation, and increases PGC1α levels in renal tissues of mice with diabetic nephropathy. LJ-2698 is applicable to the research of emphysema and diabetic nephropathy[1][2].

体外研究
(In Vitro)

LJ-2698 (0.1 μM, 72 h) 可恢复 LPS (HY-D1056) 刺激的 RAW 264.7 小鼠巨噬细胞中抗炎细胞因子 (Il4、Il10) 及 M2 型巨噬细胞标志物 (Arg1、Mrc1) 的表达[1]。

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

LJ-2698 相关抗体:

Real Time qPCR[1]

Cell Line: RAW 264.7 (murine macrophage)
Concentration: 0.1 μM
Incubation Time: 48 h (pretreatment); 24 h (co-incubation with LPS)
Result: Significantly ameliorated LPS-mediated downregulation of Il4 and Il10 anti-inflammatory cytokine mRNA expression.
Significantly restored LPS-mediated downregulation of Arg1 and Mrc1 M2 macrophage marker mRNA expression.
体内研究
(In Vivo)

LJ-2698 (50 μg/kg；灌胃；每周 6 次；持续 5 周) 可通过恢复肺功能、减少气腔扩大、抑制基质金属蛋白酶活性及肺细胞凋亡、促进 M2 巨噬细胞介导的抗炎反应，显著抑制 Elastase, Porcine pancreas (HY-P2974) 诱导的 FVB 小鼠肺气肿，且观察到的毒性极低[1]。
LJ-2698 (1.5-10 mg/kg；灌胃；每日一次；持续 12 周) 可呈剂量依赖性改善 db/db 小鼠的糖尿病肾病，其中 10 mg/kg 剂量在所有检测指标中均展现出最稳定且全面的肾脏保护作用[2]。

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

Animal Model: FVB mice (8-week-old)[1]
Dosage: 50 μg/kg
Administration: p.o.; 6 times per week; 5 weeks
Result: Restored lung compliance and tissue elasticity to levels closer to control mice.
Markedly suppressed PPE-induced airspace enlargement and reduced the elevated PPE-induced mean linear intercept (MLI).
Suppressed PPE-mediated increases in matrix metalloproteinase gelatinase activity in lung tissue.
Significantly reduced the number of TUNEL-positive apoptotic cells in the lungs compared to PPE-only treated mice.
Restored PPE-induced downregulation of anti-inflammatory cytokine (Il4, Il10) and M2 macrophage marker (Arg1, Mrc1/CD206) mRNA expression in lung tissue.
Increased the number of CD206-positive M2 macrophages per field in lung tissue.
Caused no significant changes in body weight compared to control or PPE-only groups, indicating minimal toxicity.
Animal Model: C57BLKS/J-db/db (male, 8 weeks old)[2]
Dosage: 1.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 12 weeks
Result: Significantly reduced elevated glomerular volume and fractional mesangial area across all three doses, with no significant differences between doses.
Significantly reduced increased urinary albumin excretion at 5 and 10 mg/kg doses; did not produce a significant reduction at 1.5 mg/kg dose.
Significantly prevented reduced nephrin mRNA levels and increased NGAL mRNA levels at 10 mg/kg dose.
Significantly inhibited increased TGF-β mRNA levels at 10 mg/kg dose; did not produce a significant reduction at 1.5 and 5 mg/kg doses.
Significantly reduced increased collagen IV and fibronectin mRNA levels at 5 and 10 mg/kg doses.
Significantly reduced elevated MCP-1 mRNA levels at 5 and 10 mg/kg doses; significantly inhibited increased ICAM-1 mRNA levels at 10 mg/kg dose, while 1.5 and 5 mg/kg doses did not.
Significantly decreased increased urinary LPO levels at 5 and 10 mg/kg doses.
分子量

412.29

Formula

C16H15Cl2N5O2S
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

LJ-2698 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:

LJ-2698945457-84-1LJ2698LJ 2698Adenosine ReceptorApoptosisPGC-1αP1 receptorPPARγ coactivator-1αpulmonary emphysemaFVB miceadenosine A3 receptormacrophagesRAW 264.7 murine macrophage cellsdiabetic kidney diseaseM2 macrophagemurine lung tissueMLE-12db/db mouseInhibitorinhibitorinhibit

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