Cholesterol 24-hydroxylase-IN-3
Based on 1 Customer Validation
Cholesterol 24-hydroxylase-IN-3 is an orally active, selective, and blood-brain barrier-penetrant CH24H inhibitor (IC50 = 23 nM) belonging to 1,3-oxazole derivatives. Cholesterol 24-hydroxylase-IN-3 competitively inhibits CH24H enzyme activity by using the 1,3-oxazole nitrogen atom to coordinate the heme iron and the cyclopropyl group occupying the hydrophobic pocket. Cholesterol 24-hydroxylase-IN-3 can be used for research on epilepsy and other neurological diseases.
For research use only. We do not sell to patients.
- Purity: 98.74%
- CAS No.: 1630746-27-8
- Formula: C13H10F3N3O2
- Molecular Weight:297.23
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (10 μM, 1 h) is selective for CH24H, exhibits low inhibitory rates against other CYP enzymes, with inhibitory rates of 7.3 %, 10 %, 8.5 %, and 49 % against CYP3A4, CYP2C8, CYP2C9, and CYP2D6, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6N nude female mice (7 weeks)[1]
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Dosage:30 mg/kg
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Administration:Oral gavage (i.g.), samples were collected at 1, 8, and 24 h after administration
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Result:Had excellent blood-brain barrier penetration ability (brain/plasma ratio = 1.0), and concentrations in the brain and plasma were 0.902 µM and 0.868 µM after 8 hours administration.
Significantly inhibited the CH24H enzyme function in the brain and reduced the level of cholesterol metabolite 24HC; compared to the control group, it significantly suppressed brain 24HC levels by 21%.
Chemical Information
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CAS No. 1630746-27-8
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Appearance Solid
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Molecular Weight 297.23
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Formula C13H10F3N3O2
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Color White to off-white
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SMILES
O=C(C1CC1)NC2=CC(C(F)(F)F)=CC(C3=CN=CO3)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (84.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3644 mL | 16.8220 mL | 33.6440 mL | 84.1099 mL |
| 5 mM | 0.6729 mL | 3.3644 mL | 6.7288 mL | 16.8220 mL | |
| 10 mM | 0.3364 mL | 1.6822 mL | 3.3644 mL | 8.4110 mL | |
| 15 mM | 0.2243 mL | 1.1215 mL | 2.2429 mL | 5.6073 mL | |
| 20 mM | 0.1682 mL | 0.8411 mL | 1.6822 mL | 4.2055 mL | |
| 25 mM | 0.1346 mL | 0.6729 mL | 1.3458 mL | 3.3644 mL | |
| 30 mM | 0.1121 mL | 0.5607 mL | 1.1215 mL | 2.8037 mL | |
| 40 mM | 0.0841 mL | 0.4205 mL | 0.8411 mL | 2.1027 mL | |
| 50 mM | 0.0673 mL | 0.3364 mL | 0.6729 mL | 1.6822 mL | |
| 60 mM | 0.0561 mL | 0.2804 mL | 0.5607 mL | 1.4018 mL | |
| 80 mM | 0.0421 mL | 0.2103 mL | 0.4205 mL | 1.0514 mL |