| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GSK2945 increases the transcriptional activity of Rev-erbα and a luciferase reporter with an EC50 of 2.05 μM for Bmal1, a target gene of REV-ERBs, in a dose-dependent manner[1]. Treatment of mouse and human primary hepatocytes with GSK2945 (20 μM) for 12 and 24 hours results in increased levels of Cyp7a1/CYP7A1. Treatment with GSK2945 (20 μM) also raises the mRNA and protein of Lrh-1/LRH-1, a known hepatic activator of Cyp7a1/CYP7A1[1].
|
|---|---|
| ln Vivo |
In male C57BL/6 mice, GSK2945 (0-10 mg/kg) administered intraperitoneally twice daily for seven days increases the level of hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) and decreases plasma cholesterol[1].
|
| 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.
|
| Molecular Formula |
C20H18CL2N2O2S
|
|---|---|
| Molecular Weight |
421.340121746063
|
| Exact Mass |
420.046
|
| CAS # |
1438071-12-5
|
| Related CAS # |
GSK2945 hydrochloride
|
| PubChem CID |
71682479
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
6.2
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
485
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NXCSEAQOKPSNJV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H18Cl2N2O2S/c1-14-10-18(22)7-4-16(14)12-23(11-15-2-5-17(21)6-3-15)13-19-8-9-20(27-19)24(25)26/h2-10H,11-13H2,1H3
|
| Chemical Name |
N-[(4-chloro-2-methylphenyl)methyl]-1-(4-chlorophenyl)-N-[(5-nitrothiophen-2-yl)methyl]methanamine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 83.33 mg/mL (197.77 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.94 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 | 2.3734 mL | 11.8669 mL | 23.7338 mL | |
| 5 mM | 0.4747 mL | 2.3734 mL | 4.7468 mL | |
| 10 mM | 0.2373 mL | 1.1867 mL | 2.3734 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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