ERG240 - CAS:1415683-79-2

您当前的位置：

ERG240

目录号 : KM32588 CAS No. : 1415683-79-2 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

查看所有商品（1）

加入购物车大包装询价

Other Forms of Rapamycin:

ERG240 In-stock
2,4-Dihydroxybutanoic acid In-stock
PC(O-16:0/18:2(9Z,12Z)) In-stock
S-Methyl thiomethanesulfonate In-stock
Neuraminidase, Microorganism In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

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.

体外研究

ERG240 (20 µM, 3 hours) significantly reduced the mRNA and protein levels of Irg1 in human monocyte derived macrophages and decreased the production of itaconate [2].
ERG240 (5 µM and 10 µM, 24 hours) significantly inhibited the migration of bone marrow-derived macrophages (BMDMs).

Western Blot Analysis

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

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

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

ERG240 (500 mg/kg, intraperitoneal injection (i.p.), administered 30 minutes before and 8 hours after LPS injection) significantly reduced the pro-inflammatory response and increased anti-inflammatory transcriptome features in LPS (HY-D1056) induced acute inflammation C57BL/6 mouse model.
ERG240 (720 mg/kg and 1000 mg/kg, orally administered orally (p.o.) once a day for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg) significantly alleviated inflammation and joint destruction in collagen induced arthritis DBA/1 mouse models [2].
ERG240 (500 mg/kg, orally administered orally (p.o.) once a day for 10 days) significantly reduced the severity of inflammation and renal interstitial fibrosis in the WKY rat model of nephrotoxic nephritis induced by nephrotoxic serum.

Animal Model:

LPS induced acute inflammation C57BL/6 mouse model

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 induced arthritis (CIA) DBA/1 mouse model
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
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.

分子式

C₇H₁₁NaO₃

分子量

166.15

CAS号

1415683-79-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°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

In Vitro:

H2O : 100 mg/mL (601.87 mM; Need ultrasonic)

DMSO : 25 mg/mL (150.47 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.6019 mL	3.0093 mL	6.0187 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 2.5 mg/mL (15.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (15.05 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (15.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (15.05 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 2.5 mg/mL (15.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (15.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： 98%

Data Sheet

产品使用指南

[1]. Papathanassiu, et al. Methods for treatment of cancer, inflammatory autoimmune disorders and bone diseases using branched-chain amino acid aminotransferase-1 (BCAT1) inhibitors. Patent. WO2012173987.

[2]. Papathanassiu AE, et al. BCAT1 controls metabolic reprogramming in activated human macrophages and is associated with inflammatory diseases. Nat Commun. 2017 Jul 12;8:16040.

[3]. Papathanassiu A E, et al. Inhibition of BCAT1 suppresses the expression of pro-metastatic proteins and reduces cancer metastasis[J]. Cancer Research, 2014, 74(19_Supplement): 2683-2683.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器