2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. GSK2945

GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (GSK2945 hydrochloride) that retains the same biological activity.

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

GSK2945 Chemical Structure

GSK2945 Chemical Structure

CAS No. : 1438071-12-5

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Other Forms of GSK2945:

GSK2945 Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism[1].

In Vitro

GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter (EC50 of 2.05 μM)[1].
GSK2945 (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) treatment increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes. GSK2945 (20 μM) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein[1].

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

GSK2945 Related Antibodies

RT-PCR[1]

Cell Line: Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
Concentration: 20 μM
Incubation Time: 12 hours and 24 hours
Result: Led to significant increases in mRNA and protein (at 24-h) expression of Cyp7a1. mRNA and protein (at 24-h) levels of CYP7A1 were increased in human primary hepatocyte. Lrh-1/LRH-1 was upregulated.
In Vivo

GSK2945 (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice[1].

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

Animal Model: Male C57BL/6 mice (8-10 weeks of age)[1]
Dosage: 0 mg/kg or 10 mg/kg
Administration: Intraperitoneal injection; twice every day; for 7 days
Result: Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
Molecular Weight

421.34

Formula

C20H18Cl2N2O2S
CAS No.
SMILES

O=[N+](C1=CC=C(CN(CC2=CC=C(Cl)C=C2C)CC3=CC=C(Cl)C=C3)S1)[O-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (197.77 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 2.3734 mL 11.8669 mL 23.7338 mL
5 mM 0.4747 mL 2.3734 mL 4.7468 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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 (4.94 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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% 
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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 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
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3734 mL 11.8669 mL 23.7338 mL 59.3345 mL
5 mM 0.4747 mL 2.3734 mL 4.7468 mL 11.8669 mL
10 mM 0.2373 mL 1.1867 mL 2.3734 mL 5.9335 mL
15 mM 0.1582 mL 0.7911 mL 1.5823 mL 3.9556 mL
20 mM 0.1187 mL 0.5933 mL 1.1867 mL 2.9667 mL
25 mM 0.0949 mL 0.4747 mL 0.9494 mL 2.3734 mL
30 mM 0.0791 mL 0.3956 mL 0.7911 mL 1.9778 mL
40 mM 0.0593 mL 0.2967 mL 0.5933 mL 1.4834 mL
50 mM 0.0475 mL 0.2373 mL 0.4747 mL 1.1867 mL
60 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9889 mL
80 mM 0.0297 mL 0.1483 mL 0.2967 mL 0.7417 mL
100 mM 0.0237 mL 0.1187 mL 0.2373 mL 0.5933 mL
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GSK2945 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:

GSK29451438071-12-5GSK 2945GSK-2945Cytochrome P450CYPsInhibitorinhibitorinhibit

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