2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. TP-020

TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

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

TP-020 Chemical Structure

TP-020 Chemical Structure

CAS No. : 1800025-30-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 777 In-stock
Solution
10 mM * 1 mL in DMSO USD 777 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 540 In-stock
10 mg USD 900 In-stock
25 mg USD 1800 In-stock
50 mg USD 2640 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

TP-020 Related Antibodies

Top Publications Citing Use of Products

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ACAT1 ACAT2 MGAT2 ACAT

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TP-020 (MGAT2-IN-1) is an orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.

IC50 & Target

IC50: 7.8 nM (Human MGAT2), 2.4 nM (Mouse MGAT2)[1]
In Vivo

TP-020 (3, 10 mg/kg, p.o.) dose-dependently suppresses plasma TG elevation, and plasma CM/TG AUC in mice. TP-020 does not decrease MG absorption but inhibits MGAT2-dependent TG/DG resynthesis. In the lipid utilization analysis, TP-020 significantly increases free fatty acid (FFA) and acylcarnitine levels. TP-020 (30 mg/kg) also significantly reduces food intake dose dependently, suppresses BW gains. TP-020 shows anti-diabetic effects in mice[1].

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

654.01

Formula

C27H21ClF5N7O3S
CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=S(C1=CC2=C(N(C3=NC=C(C4=CC(C(F)(F)F)=NN4C)C=N3)CC2)C(N5C(CCC5)=O)=C1)(NC6=C(F)C=C(Cl)C=C6F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (191.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5290 mL 7.6451 mL 15.2903 mL
5 mM 0.3058 mL 1.5290 mL 3.0581 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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 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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Mice: Overnight-fasted mice undergo MTT in the morning. First, they are orally administered vehicle (0.5% methylcellulose solution) or MGAT2-IN-1 suspended in 0.5% methylcellulose. Six or 16 h after dosing, they are intraperitoneally injected 500 mg/kg Pluronic F-127 to inhibit plasma TG hydrolysis by lipoprotein lipase (LPL). Thirty minutes after injection, the mice are given an oral liquid meal (10 mL/kg) comprising an admixture of corn oil and Ensure-H (3:17 v/v). Blood samples are collected at 0, 2 and 4 h after oral gavage of the liquid meal. Area under the curve (AUC) of chylomicron TG (CM/TG), which is synthesised from dietary fat in the small intestine, is calculated by subtracting plasma TG levels of a liquid meal-untreated group from plasma TG levels of each treated group.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5290 mL 7.6451 mL 15.2903 mL 38.2257 mL
5 mM 0.3058 mL 1.5290 mL 3.0581 mL 7.6451 mL
10 mM 0.1529 mL 0.7645 mL 1.5290 mL 3.8226 mL
15 mM 0.1019 mL 0.5097 mL 1.0194 mL 2.5484 mL
20 mM 0.0765 mL 0.3823 mL 0.7645 mL 1.9113 mL
25 mM 0.0612 mL 0.3058 mL 0.6116 mL 1.5290 mL
30 mM 0.0510 mL 0.2548 mL 0.5097 mL 1.2742 mL
40 mM 0.0382 mL 0.1911 mL 0.3823 mL 0.9556 mL
50 mM 0.0306 mL 0.1529 mL 0.3058 mL 0.7645 mL
60 mM 0.0255 mL 0.1274 mL 0.2548 mL 0.6371 mL
80 mM 0.0191 mL 0.0956 mL 0.1911 mL 0.4778 mL
100 mM 0.0153 mL 0.0765 mL 0.1529 mL 0.3823 mL
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TP-020 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:

TP-0201800025-30-2MGAT2-IN-1TP020TP 020AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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