1. Metabolic Enzyme/Protease
  2. ATP Citrate Lyase
  3. EVT0185

EVT0185 是一种口服有效的 ATP 柠檬酸裂解酶 (ACLY) 抑制剂。EVT0185 在肝脏中被 SLC27A2 转化为 CoA 硫酯,并与 ACLY 的 CoA 结合位点相互作用。EVT0185-CoA 抑制 ACLY 活性,IC50 值为 2.5 μM。EVT0185 能模拟 ACLY 基因缺失产生的免疫和抗肿瘤效应。EVT0185 可增加肿瘤浸润性 B 细胞和趋化因子 CXCL13 的水平。EVT0185 可用于癌症研究,如肝细胞癌 (HCC)。

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EVT0185

EVT0185 Chemical Structure

CAS No. : 2588489-03-4

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5 mg ¥6080
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EVT0185 is an orally active ATP citrate lyase (ACLY) inhibitor. EVT0185 is converted to a CoA thioester in the liver by SLC27A2 and interacts with the CoA-binding site of ACLY. EVT0185-CoA inhibits ACLY activity with an IC50 of 2.5 μM. EVT0185 can phenocopy the immune and antitumour effects of genetic ACLY deletion. EVT0185 can increase tumour-infiltrating B cells and chemokine CXCL13 levels. EVT0185 can be used for the research of cancer, such as hepatocellular carcinoma (HCC)[1].

体外研究
(In Vitro)

EVT0185 抑制肝细胞中的脂肪生成,IC50 值为 0.46 μM[1]

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

体内研究
(In Vivo)

EVT0185 (30-100 mg/kg,灌胃给药,持续 1 个月) 可减轻 MASH-HCC 小鼠模型中的肿瘤负荷[1]

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

Animal Model: Metabolic dysfunction-associated steatohepatitis (MASH)-driven hepatocellular carcinoma (HCC) mice models[1]
Dosage: 30 and 100 mg/kg
Administration: Orally gavaged, 1 month
Result: Reduced tumor numbers in liver.
Reduced tumour surface area and lipid accumulation.
Elevated levels of AFP.
Increased B cells and B cell chemoattractant CXCL13 levels.
Increased cleaved caspase 3 levels and reduced Ki67 levels.
分子量

362.50

Formula

C22H34O4

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
  • 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.

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产品名称:
EVT0185
目录号:
HY-175606
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