GSK2945
Based on 1 publication(s) in Google Scholar
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.
- CAS No.: 1438071-12-5
- Formula: C20H18Cl2N2O2S
- Molecular Weight:421.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GSK2945
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Biological Activity
Description
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.
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Cell Line:Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
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Concentration:20 μM
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Incubation Time:12 hours and 24 hours
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8-10 weeks of age)[1]
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Dosage:0 mg/kg or 10 mg/kg
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Administration:Intraperitoneal injection; twice every day; for 7 days
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Result:Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.
Chemical Information
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CAS No. 1438071-12-5
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Molecular Weight 421.34
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Formula C20H18Cl2N2O2S
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SMILES
O=[N+](C1=CC=C(CN(CC2=CC=C(Cl)C=C2C)CC3=CC=C(Cl)C=C3)S1)[O-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Electroacupuncture alleviates acute gouty arthritis by inhibiting NLRP3 inflammasome activation via modulation of the circadian-inflammation axis. [Abstract]2026 Jun 15:179:116650. PMID: 41967209
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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 |
GSK2945 Related Classifications
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