2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Cholesterol 24-hydroxylase-IN-3

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[1].

For research use only. We do not sell to patients.

Cholesterol 24-hydroxylase-IN-3 Chemical Structure

Cholesterol 24-hydroxylase-IN-3 Chemical Structure

CAS No. : 1630746-27-8

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Cholesterol 24-hydroxylase-IN-3 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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Description

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[1].

In Vitro

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.

Cholesterol 24-hydroxylase-IN-3 Related Antibodies
In Vivo

Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (30 mg/kg, i.g, single dose) can effectively penetrate the blood-brain barrier and reduce the level of 24S-hydroxycholesterol (24HC) in the brain in mice, providing a new treatment strategy for neurological diseases[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6N nude female mice (7 weeks)[1]
Dosage: 30 mg/kg
Administration: Oral gavage (i.g.), samples were collected at 1, 8, and 24 h after administration
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%.
Molecular Weight

297.23

Formula

C13H10F3N3O2
CAS No.
SMILES

O=C(C1CC1)NC2=CC(C(F)(F)F)=CC(C3=CN=CO3)=N2
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Cholesterol 24-hydroxylase-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cholesterol 24-hydroxylase-IN-31630746-27-8Cytochrome P450CYPsEpilepsyC57BL/6N nude miceFreeStyle 293-F cells1,3,4-oxadiazoleCH24HInhibitorinhibitorinhibit

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