| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
GSK2945 hydrochloride increases, in a dose-dependent manner (EC50 = 2.05 μM), the transcriptional activity of the Rev-erbα and Bmal1 (the target gene of REV-ERB) luciferase reporter genes. [1]. Cyp7a1/CYP7A1 levels in mouse and human primary hepatocytes are increased by treatment with GSK2945 hydrochloride (20 μM; 12 hours and 24 hours). Treatment with GSK2945 hydrochloride (20 μM) also raises the levels of Lrh-1/LRH-1 mRNA and protein, which is a recognized hepatic activator of Cyp7a1/CYP7A1 [1].
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| ln Vivo |
GSK2945 hydrochloride (0–10 mg/kg; intraperitoneal; twice daily for 7 days; male C57BL/6 mice) treatment lowered wild-type plasma cholesterol in rats and elevated mouse liver cholesterol 7α-hydroxylase (Cyp7a1) levels [1].
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| Cell Assay |
RT-PCR[1]
Cell Types: Mouse(male, CD1) and human(male, Caucasian) primary hepatocytes Tested Concentrations: 20 μM Incubation Duration: 12 hrs (hours) and 24 hrs (hours) Experimental Results: 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. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (8-10 weeks of age)[1]
Doses: 0 mg/kg or 10 mg/kg Route of Administration: intraperitoneal (ip)injection; twice every day; for 7 days Experimental Results: Increased hepatic mouse cholesterol 7α- hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice. |
| References |
[1]. Zhang T, et al. REV-ERBα Regulates CYP7A1 Through Repression of Liver Receptor Homolog-1. Drug Metab Dispos. 2018 Mar;46(3):248-258.
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| Molecular Formula |
C20H19CL3N2O2S
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|---|---|
| Molecular Weight |
457.80
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| Related CAS # |
GSK2945;1438071-12-5
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~20.83 mg/mL (~45.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.54 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1844 mL | 10.9218 mL | 21.8436 mL | |
| 5 mM | 0.4369 mL | 2.1844 mL | 4.3687 mL | |
| 10 mM | 0.2184 mL | 1.0922 mL | 2.1844 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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