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ERG240 是一种具有口服活性的支链氨基酸转氨酶 1 (BCAT1) 抑制剂。EGR240 可用于癌症、类风湿性关节炎和骨病的研究。

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ERG240 Chemical Structure

ERG240 Chemical Structure

CAS No. : 1415683-79-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1980
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25 mg ¥1800
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50 mg ¥3000
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100 mg ¥4700
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500 mg   询价  

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Customer Review

MCE 顾客使用本产品发表的 2 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ERG240 is an oral active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. ERG240 can be used for the research of cancer, rheumatoid arthritis, and bone disease[1].

体外研究
(In Vitro)

ERG240(20 µM,3 小时)显著降低了人类单核细胞衍生巨噬细胞中 Irg1 的 mRNA 和蛋白水平,并减少了 itaconate 的生成 [2]
ERG240(5 µM 和 10 µM,24 小时)显著抑制了骨髓衍生巨噬细胞(BMDMs)的迁移 [2]

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

Western Blot Analysis[2]

Cell Line: Human monocyte-derived macrophages (hMDMs)
Concentration: 20 µM
Incubation Time: 3 hours
Result: Resulted in a significant reduction in IRG1 and IL-1β protein levels, with no significant change in HIF1A and ACTB expression.

Cell Migration Assay [2]

Cell Line: Bone Marrow-Derived Macrophages (BMDMs)
Concentration: 5 µM and 10 µM
Incubation Time: 24 hours
Result: Inhibited BMDM migration in a dose-dependent manner without affecting cell viability.

Real Time qPCR[2]

Cell Line: Human monocyte-derived macrophages (hMDMs)
Concentration: 20 µM
Incubation Time: 3 hours
Result: Significantly reduced Irg1 mRNA levels, along with itaconate production, without affecting HIF1A and IL1B mRNA levels.
体内研究
(In Vivo)

ERG240(500 mg/kg,腹腔注射 (i.p.),在 LPS 注射前 30 分钟和后 8 小时给药)显著降低了 LPS (HY-D1056) 诱导的急性炎症 C57BL/6 小鼠模型中的促炎反应,并增加了抗炎转录组特征 [2]
ERG240(720 mg/kg 和 1000 mg/kg,口服灌胃 (p.o.),每天一次,分别持续 3 周 (720 mg/kg) 和 4 周 (1000 mg/kg))显著缓解了胶原诱导的关节炎 DBA/1 小鼠模型中的炎症和关节破坏 [2]
ERG240(500 mg/kg,口服灌胃 (p.o.),每天一次,持续 10 天)显著减轻了肾毒性血清诱导的肾毒性肾炎 WKY 大鼠模型中的炎症严重程度和肾间质纤维化 [2]

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

Animal Model: LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2]
Dosage: 500 mg/kg
Administration: Intraperitoneal injection (i.p.), administered 30 min before and 8 h after LPS injection
Result: Reduced Irg1 mRNA and protein levels along with itaconate production.
Animal Model: Collagen (HY-NP102)-induced arthritis (CIA) DBA/1 mouse model[2]
Dosage: 720 and 1000 mg/kg
Administration: Oral gavage (p.o.), once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg)
Result: Significantly reduced inflammation, cartilage damage, pannus formation, and bone resorption in CIA model; decreased serum levels of pro-inflammatory markers TNF and RANKL.
Animal Model: Nephrotoxic nephritis (NTN) WKY rat model induced by nephrotoxic serum (NTS) injection[2]
Dosage: 500 mg/kg
Administration: Oral gavage (p.o.), once daily for 10 days
Result: Reduced glomerular crescent formation, proteinuria, serum creatinine, and collagen type I levels.
分子量

166.15

Formula

C7H11NaO3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (601.87 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 100 mg/mL (601.87 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.0187 mL 30.0933 mL 60.1866 mL
5 mM 1.2037 mL 6.0187 mL 12.0373 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 6.0187 mL 30.0933 mL 60.1866 mL 150.4665 mL
5 mM 1.2037 mL 6.0187 mL 12.0373 mL 30.0933 mL
10 mM 0.6019 mL 3.0093 mL 6.0187 mL 15.0466 mL
15 mM 0.4012 mL 2.0062 mL 4.0124 mL 10.0311 mL
20 mM 0.3009 mL 1.5047 mL 3.0093 mL 7.5233 mL
25 mM 0.2407 mL 1.2037 mL 2.4075 mL 6.0187 mL
30 mM 0.2006 mL 1.0031 mL 2.0062 mL 5.0155 mL
40 mM 0.1505 mL 0.7523 mL 1.5047 mL 3.7617 mL
50 mM 0.1204 mL 0.6019 mL 1.2037 mL 3.0093 mL
60 mM 0.1003 mL 0.5016 mL 1.0031 mL 2.5078 mL
80 mM 0.0752 mL 0.3762 mL 0.7523 mL 1.8808 mL
100 mM 0.0602 mL 0.3009 mL 0.6019 mL 1.5047 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
ERG240
目录号:
HY-W193545A
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