| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
Imanixil targets the LDL receptor (LDLR) pathway. It is an inducer of the LDL receptor, enhancing its expression and promoting hepatic clearance of circulating LDL cholesterol. By increasing LDLR expression, it improves lipid metabolism and lowers cholesterol levels. It may also act as a PIP5K2B inhibitor, although its primary mechanism is related to LDLR induction.
|
|---|---|
| ln Vitro |
Imanixil is an inducer of the LDL receptor (LDLR). It is a potent cholesterol-lowering agent that enhances LDLR expression and promotes hepatic clearance of circulating LDL cholesterol. Its activity has been confirmed in various in vitro and in vivo studies. As an LDLR inducer, it contributes to improved lipid metabolism. It may also act as a PIP5K2B inhibitor.
|
| ln Vivo |
Imanixil is a potent cholesterol-lowering agent and inducer of the LDL receptor (LDLR). By enhancing LDLR expression, it promotes hepatic clearance of circulating LDL cholesterol, contributing to improved lipid metabolism. It has been investigated as an experimental drug for the treatment of hypercholesterolemia and related metabolic disorders.
|
| Enzyme Assay |
The primary in vitro assay for Imanixil measures its ability to induce LDL receptor expression in cultured cells, such as hepatocytes. Cells are treated with the compound, and LDLR mRNA and protein levels are measured by qPCR and Western blot. LDL uptake assays are performed using fluorescently labeled LDL to assess the functional activity of the induced receptors. Its effects on cholesterol synthesis and metabolism are also assessed.
|
| Cell Assay |
In vitro cellular experiments for Imanixil involve treating hepatocytes or other cell types with the compound and measuring its effects on LDLR expression, LDL uptake, and cholesterol metabolism. The induction of LDLR expression is assessed at the mRNA and protein levels. The functional activity of the induced receptors is assessed by measuring the uptake of labeled LDL. The compound's effects on cellular cholesterol levels are also measured.
|
| Animal Protocol |
In vivo animal experiments for Imanixil involve administering the compound to animal models of hypercholesterolemia, such as LDL receptor-deficient mice or diet-induced models. The compound's effects on serum cholesterol levels, LDL clearance, and lipid metabolism are assessed. Its effects on liver LDLR expression are also evaluated. These studies confirm its cholesterol-lowering efficacy.
|
| ADME/Pharmacokinetics |
Imanixil has a molecular weight of 394.35 and a molecular formula of C17H17F3N6O2. It is a small molecule drug with a CAS number of 75689-93-9. The compound is an inducer of the LDL receptor (LDLR) and a potent cholesterol-lowering agent. It is an experimental compound that is not approved for clinical use.
|
| Toxicity/Toxicokinetics |
Imanixil is a research compound that is not intended for human use. Its toxicological profile is not extensively characterized in the available literature. As a cholesterol-lowering agent, its safety would need to be evaluated in preclinical and clinical studies. Its effects on lipid metabolism and potential off-target effects would be assessed.
|
| References | |
| Additional Infomation |
Imanixil (HOE-402 free base) is an inducer of the LDL receptor (LDLR) and a potent cholesterol-lowering agent. By enhancing LDLR expression, it promotes hepatic clearance of circulating LDL cholesterol, contributing to improved lipid metabolism. It may also act as a PIP5K2B inhibitor. Imanixil is an experimental compound with a CAS number of 75689-93-9.
|
| Molecular Formula |
C17H17F3N6O2
|
|---|---|
| Molecular Weight |
394.36
|
| Exact Mass |
394.137
|
| CAS # |
75689-93-9
|
| PubChem CID |
216289
|
| Appearance |
White to off-white solid powder
|
| Density |
1.428g/cm3
|
| Index of Refraction |
1.601
|
| LogP |
3.686
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
614
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FUSNOPLQVRUIIM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H17F3N6O2/c1-16(2)8-26(15(28)25-16)14-22-7-11(12(21)24-14)13(27)23-10-5-3-4-9(6-10)17(18,19)20/h3-7H,8H2,1-2H3,(H,23,27)(H,25,28)(H2,21,22,24)
|
| Chemical Name |
4-amino-2-(4,4-dimethyl-2-oxoimidazolidin-1-yl)-N-[3-(trifluoromethyl)phenyl]pyrimidine-5-carboxamide
|
| Synonyms |
SAR088; SAR 088; SAR-088
|
| 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 : ~100 mg/mL (~253.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 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 (5.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5358 mL | 12.6788 mL | 25.3575 mL | |
| 5 mM | 0.5072 mL | 2.5358 mL | 5.0715 mL | |
| 10 mM | 0.2536 mL | 1.2679 mL | 2.5358 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
