2. Metabolic Enzyme/Protease GPCR/G Protein NF-κB Immunology/Inflammation Apoptosis
  3. Carboxylesterase (CES) Free Fatty Acid Receptor Reactive Oxygen Species (ROS) Mitochondrial Metabolism Ferroptosis Apoptosis
  4. GR148672X

GR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis.

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

GR148672X

GR148672X Chemical Structure

CAS No. : 263890-70-6

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GR148672X Related Antibodies

Top Publications Citing Use of Products

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CES1 CES2 CES3

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FFAR1 FFAR2 FFAR3 FFAR4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis[1][2].

IC50 & Target

IC50: 4 nM (TGH)[1]
In Vitro

GR148672X (10 μM; 4 days) potently reduces the viability of CT-26 colorectal cancer cells under glucose-restricted conditions, with no significant toxicity observed under normal glucose conditions[1].
GR148672X (10 μM; 4 days) potently reduces the viability of human colorectal cancer cell lines HCT-116, RKO, HT-29, CaCo-2, LS1034, and LS174T under glucose-restricted conditions, while showing no significant toxicity under normal glucose conditions[1].
GR148672X (10 µM; 5 h) reduces the secretion of stored triacylglycerol by 46% in primary rat hepatocytes[2].
GR148672X (10 µM; 4 h) reduces apoB-100 secretion by 42% and apoB-48 secretion by 20% in primary rat hepatocytes, without altering apoB synthesis, total protein secretion, or cell viability[2].

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

GR148672X Related Antibodies

Cell Viability Assay[1]

Cell Line: murine CT-26 colorectal carcinoma (CRC) cells
Concentration: 10 μM
Incubation Time: 4 days
Result: Showed no overt toxicity under normal glucose conditions.
Significantly increased glucose limitation-induced cell death, reducing cell survival to less than 10% of vehicle-treated control cells under glucose limitation.

Cell Viability Assay[1]

Cell Line: HCT-116, RKO, HT-29, CaCo-2, LS1034, LS174T human CRC cell lines
Concentration: 10 μM
Incubation Time: 4 days
Result: Significantly increased glucose limitation-induced cell death in all six human CRC cell lines tested, reducing cell survival to 5% or less of vehicle-treated control cells under glucose limitation.
Showed no overt toxicity under normal culture conditions.
In Vivo

GR148672X (50 mg/kg; i.p.; once daily for 10-27 days) significantly inhibits the in vivo tumorigenesis and progression of colorectal cancer, and exhibits good tolerability.

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

Animal Model: CT-26 and CHT-116 CRC allograft mice[1]
Dosage: 50 mg/kg
Administration: i.p.; once daily for 10 (CT-26) or 27 (HCT-116) days
Result: Showed a significant effect in inhibiting tumor growth, and there was no obvious toxic reactions.
Molecular Weight

340.32

Formula

C15H11F3N2O2S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CS1)/C(C(C(F)(F)F)=O)=N\NC2=CC=CC(C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (122.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9384 mL 14.6921 mL 29.3841 mL
5 mM 0.5877 mL 2.9384 mL 5.8768 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (6.11 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*The compound is unstable in solutions, freshly prepared is recommended.

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.58%

SDS (393 KB)

COA (252 KB) HNMR (219 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9384 mL 14.6921 mL 29.3841 mL 73.4603 mL
5 mM 0.5877 mL 2.9384 mL 5.8768 mL 14.6921 mL
10 mM 0.2938 mL 1.4692 mL 2.9384 mL 7.3460 mL
15 mM 0.1959 mL 0.9795 mL 1.9589 mL 4.8974 mL
20 mM 0.1469 mL 0.7346 mL 1.4692 mL 3.6730 mL
25 mM 0.1175 mL 0.5877 mL 1.1754 mL 2.9384 mL
30 mM 0.0979 mL 0.4897 mL 0.9795 mL 2.4487 mL
40 mM 0.0735 mL 0.3673 mL 0.7346 mL 1.8365 mL
50 mM 0.0588 mL 0.2938 mL 0.5877 mL 1.4692 mL
60 mM 0.0490 mL 0.2449 mL 0.4897 mL 1.2243 mL
80 mM 0.0367 mL 0.1837 mL 0.3673 mL 0.9183 mL
100 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7346 mL
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GR148672X 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:

GR148672X263890-70-6Carboxylesterase (CES)Free Fatty Acid ReceptorReactive Oxygen Species (ROS)Mitochondrial MetabolismFerroptosisApoptosisCarboxylesteraseCarboxylic-ester HydrolaseFFARcarboxylesterase 1pancreatic lipasecolorectal cancer cellCT-26 CRC cellhepatic microsomal triacylglycerol hydrolaselipoprotein lipasehormone-sensitive lipaseprimary rat hepatocytesacetylcholine esterasemouse colorectal carcinoma modelsInhibitorinhibitorinhibit

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