2. Membrane Transporter/Ion Channel
  3. URAT1
  4. HYJ-2

HYJ-2 是一种 URAT1 抑制剂与降尿酸剂。HYJ-2 可抑制 URAT1 介导的尿酸转运，并与 URAT1 结合口袋内的关键残基发生相互作用。HYJ-2 可降低高尿酸血症小鼠的血清尿酸水平，且不会诱发肝损伤或肾损伤。HYJ-2 对肝细胞和肾细胞的细胞毒性较低。HYJ-2 不会显著诱导肝细胞凋亡或线粒体功能障碍。HYJ-2 可用于高尿酸血症、痛风的相关研究。

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HYJ-2

HYJ-2 Chemical Structure

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HYJ-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HYJ-2 is a URAT1 inhibitor and urate-lowering agent. HYJ-2 inhibits URAT1-mediated urate transport and interacts with key residues within the URAT1 binding pocket. HYJ-2 reduces serum urate levels in hyperuricemic mice without inducing liver or kidney injury. HYJ-2 shows low cytotoxicity to hepatocytes and renal cells. HYJ-2 does not significantly induce hepatocyte apoptosis or mitochondrial dysfunction. HYJ-2 can be used in studies related to hyperuricemia and gout[1].

体外研究
(In Vitro)

HYJ-2 (10-10000 nM) 可强效抑制过表达 URAT1 的 HEK293 细胞中 URAT1 介导的尿酸盐摄取，其 IC50 为 368 nM[1]。
HYJ-2 对 HEK293T 细胞的细胞毒性较低，其 IC50 为 353.1 μM[1]。
HYJ-2 对 HepG2 细胞表现出低细胞毒性，其 IC50 为 287.3 μM[1]。
HYJ-2 (100 μM; 24 h) 不会显著促进 HepG2 细胞的凋亡[1]。
HYJ-2 (100 μM; 24 h) 对 HepG2 细胞的线粒体功能影响较弱，73.7% 的细胞仍保持较高的线粒体膜电位[1]。
HYJ-2 在人肝微粒体中表现出优异的代谢稳定性，半衰期为 990 min，孵育 60 min 后仍有 97.3% 的母药残留[1]。

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

HYJ-2 相关抗体:

Apoptosis Analysis[1]

Cell Line: human hepatocellular carcinoma HepG2 cells
Concentration: 100 μM
Incubation Time: 24 h
Result: Induced an apoptotic rate of 5.6% in HepG2 cells, which was comparable to the control group.
体内研究
(In Vivo)

HYJ-2 (2 mg/kg；19 天) 可使高尿酸血症雄性昆明小鼠的血清尿酸水平降低 36.7%，同时缓解高尿酸血症相关肾损伤，且未引发明显的肝损伤[1]。

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

Animal Model: Kunming mice with Hyperuricemia (male, 19-21 g)[1]
Dosage: 2 mg/kg
Administration: 19 days
Result: Reduced mean serum uric acid levels from 1042.3 μM to 683.3 μM, corresponding to a 36.7% decrease rate.
Alleviated renal pathological injury associated with long-term hyperuricemia, with better preservation of renal tubular architecture and a more pronounced reduction in interstitial inflammatory cell infiltration than the reference drug group.
Showed no apparent hepatic pathological abnormalities.
分子量

322.15

Formula

C14H9Cl2N3O2
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

HYJ-2 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:

HYJ-2HYJ2HYJ 2URAT1Urate transporter 1SLC22A12hepatic cellshyperuricemic miceapoptosisgoutHEK293 cellsmitochondrial dysfunctionrenal cellsHepG2 cellshyperuricemiaInhibitorinhibitorinhibit

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