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

Cholesterol 24-hydroxylase-IN-3 是一种口服有效，具有选择性并能穿过血脑屏障的 CH24H 抑制剂(IC50 = 23 nM)，属于 1,3-恶唑衍生物。Cholesterol 24-hydroxylase-IN-3 通过1,3-恶唑氮原子与血红素铁配位，环丙基占据疏水口袋竞争性抑制 CH24H 酶活性。Cholesterol 24-hydroxylase-IN-3 可用于癫痫等神经系统疾病的研究[1]。

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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 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (10 μM, 1 h) 对 CH24H 具有选择性，对其它 CYP 酶抑制率低，对 CYP3A4、CYP2C8、CYP2C9 和 CYP2D6 抑制率分别为 7.3 %、10 %、8.5 % 和 49 %[1]。

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

Cholesterol 24-hydroxylase-IN-3 相关抗体:
体内研究
(In Vivo)

Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (30 mg/kg, i.g, 单剂量) 在小鼠中能有效穿透血脑屏障，且降低脑内 24S-羟基胆固醇 (24HC) 水平，为神经疾病提供新治疗策略[1]。

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%.
分子量

297.23

Formula

C13H10F3N3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Cholesterol 24-hydroxylase-IN-3 相关分类

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  • 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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