1. Metabolic Enzyme/Protease
  2. Acyltransferase
  3. H2-003

H2-003 is a diacylglycerol acyltransferase DGAT2 inhibitor with an IC50 value of 7.4 μM against human targets. H2-003 reduces triacylglycerol biosynthesis and inhibits lipid droplet formation. H2-003 can be used in studies related to hepatic steatosis and insulin resistance.

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H2-003

H2-003 Chemical Structure

CAS No. : 1060438-30-3

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Description

H2-003 is a diacylglycerol acyltransferase DGAT2 inhibitor with an IC50 value of 7.4 μM against human targets. H2-003 reduces triacylglycerol biosynthesis and inhibits lipid droplet formation. H2-003 can be used in studies related to hepatic steatosis and insulin resistance[1].

IC50 & Target

DGAT2[1].

In Vitro

H2-003 inhibits lipid droplet formation with an IC50 of 5 μM in DGAT2-overexpressing HEK293 Tet-on cells, but has minimal effect on DGAT1-overexpressing HEK293 Tet-on cells[1].
H2-003 (1-10 μM; 48 h) suppresses oleic acid-induced lipid droplet formation in 3T3-L1 cells in a dose-dependent manner, and co-treatment with a DGAT1 inhibitor at 10 μM nearly eliminates lipid droplet formation entirely[1].

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

Molecular Weight

446.50

Formula

C25H26N4O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(NC(C2=CC=CC=C2)=O)C3=CC(NC(C)CC)=CN=C3N1CC4=CC=CO4)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (279.96 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 2.2396 mL 11.1982 mL 22.3964 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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. 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 1 mM 2.2396 mL 11.1982 mL 22.3964 mL 55.9910 mL
5 mM 0.4479 mL 2.2396 mL 4.4793 mL 11.1982 mL
10 mM 0.2240 mL 1.1198 mL 2.2396 mL 5.5991 mL
15 mM 0.1493 mL 0.7465 mL 1.4931 mL 3.7327 mL
20 mM 0.1120 mL 0.5599 mL 1.1198 mL 2.7996 mL
25 mM 0.0896 mL 0.4479 mL 0.8959 mL 2.2396 mL
30 mM 0.0747 mL 0.3733 mL 0.7465 mL 1.8664 mL
40 mM 0.0560 mL 0.2800 mL 0.5599 mL 1.3998 mL
50 mM 0.0448 mL 0.2240 mL 0.4479 mL 1.1198 mL
60 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.6999 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5599 mL
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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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Product Name:
H2-003
Cat. No.:
HY-23199
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