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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.

For research use only. We do not sell to patients.

ERG240 Chemical Structure

ERG240 Chemical Structure

CAS No. : 1415683-79-2

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25 mg USD 180 In-stock
50 mg USD 300 In-stock
100 mg USD 470 In-stock
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500 mg   Get quote  

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Based on 2 publication(s) in Google Scholar

ERG240 Related Antibodies

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Description

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].

In Vitro

ERG240 (20 µM, 3 hours) significantly reduces Irg1 mRNA and protein levels, along with itaconate production, in human monocyte-derived macrophages[2].
ERG240 (5 µM and 10 µM, 24 hours) significantly inhibits migration in bone marrow-derived macrophages (BMDMs)[2].

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

ERG240 Related Antibodies

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.
In Vivo

ERG240 (500 mg/kg, i.p., administered 30 min before and 8 h after LPS injection) significantly decreases pro-inflammatory response and increases anti-inflammatory transcriptomic features in LPS (HY-D1056)-induced acute inflammation C57BL/6 mouse model[2].
ERG240 (720 mg/kg and 1000 mg/kg, p.o., once daily for 3 weeks (720 mg/kg) and 4 weeks (1000 mg/kg)) significantly alleviates inflammation and joint destruction in the collagen-induced arthritis DBA/1 mouse model[2].
ERG240 (500 mg/kg, p.o., once daily for 10 days) significantly reduces the severity of inflammation and interstitial fibrosis in the NTN WKY rat model induced by nephrotoxic serum[2].

MedChemExpress (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.
Molecular Weight

166.15

Formula

C7H11NaO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCC(C)C(C)=O)O[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (601.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

SDS (252 KB)

COA (244 KB) HNMR (256 KB) MS (178 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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ERG240 Related Classifications

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:

ERG2401415683-79-2ERG 240ERG-240Othersbranched-chain amino acid aminotransferase 1 (BCAT1)cancerrheumatoid arthritisbone diseaseInhibitorinhibitorinhibit

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