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Cholesterol 24-hydroxylase-IN-3

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Catalog No. T210815Cas No. 1630746-27-8

Cholesterol24-hydroxylase-IN-3 is an orally bioavailable, selective, brain-penetrant CH24H inhibitor (IC50 = 23 nM), classified as a 1,3-oxazole derivative. It inhibits CH24H enzyme activity competitively by coordinating the 1,3-oxazole nitrogen atom with the heme iron, with the cyclopropyl group occupying a hydrophobic pocket. Cholesterol24-hydroxylase-IN-3 has potential applications in research on neurological disorders like epilepsy.

Cholesterol 24-hydroxylase-IN-3

Cholesterol 24-hydroxylase-IN-3

😃Good
Catalog No. T210815Cas No. 1630746-27-8
Cholesterol24-hydroxylase-IN-3 is an orally bioavailable, selective, brain-penetrant CH24H inhibitor (IC50 = 23 nM), classified as a 1,3-oxazole derivative. It inhibits CH24H enzyme activity competitively by coordinating the 1,3-oxazole nitrogen atom with the heme iron, with the cyclopropyl group occupying a hydrophobic pocket. Cholesterol24-hydroxylase-IN-3 has potential applications in research on neurological disorders like epilepsy.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mgInquiry10-14 weeks10-14 weeks
50 mgInquiry10-14 weeks10-14 weeks
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Product Introduction

Bioactivity
Description
Cholesterol24-hydroxylase-IN-3 is an orally bioavailable, selective, brain-penetrant CH24H inhibitor (IC50 = 23 nM), classified as a 1,3-oxazole derivative. It inhibits CH24H enzyme activity competitively by coordinating the 1,3-oxazole nitrogen atom with the heme iron, with the cyclopropyl group occupying a hydrophobic pocket. Cholesterol24-hydroxylase-IN-3 has potential applications in research on neurological disorders like epilepsy.
In vitro
Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (10 μM, 1 h) selectively inhibits CH24H while exhibiting minimal inhibition of other CYP enzymes, with inhibition rates of 7.3% for CYP3A4, 10% for CYP2C8, 8.5% for CYP2C9, and 49% for CYP2D6.
In vivo
Cholesterol 24-hydroxylase-IN-3 (Compound 4L) at a dose of 30 mg/kg (i.g, single dose) effectively crosses the blood-brain barrier in mice and reduces levels of 24S-hydroxycholesterol (24HC) in the brain, offering a novel therapeutic approach for neurological disorders.
Chemical Properties
Molecular Weight297.23
FormulaC13H10F3N3O2
Cas No.1630746-27-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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