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Cholesterol24-hydroxylase-IN-3 是一种选择性强、能穿过血脑屏障的口服 CH24H 抑制剂 (IC50= 23 nM),归属于 1,3-恶唑衍生物。Cholesterol24-hydroxylase-IN-3 通过其1,3-恶唑氮原子与血红素铁结合,同时环丙基占据疏水口袋,竞争性抑制CH24H酶的活性。用于研究癫痫等神经系统疾病。

Cholesterol24-hydroxylase-IN-3 是一种选择性强、能穿过血脑屏障的口服 CH24H 抑制剂 (IC50= 23 nM),归属于 1,3-恶唑衍生物。Cholesterol24-hydroxylase-IN-3 通过其1,3-恶唑氮原子与血红素铁结合,同时环丙基占据疏水口袋,竞争性抑制CH24H酶的活性。用于研究癫痫等神经系统疾病。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 10 mg | 待询 | 10-14周 | |
| 50 mg | 待询 | 10-14周 |
Cholesterol 24-hydroxylase-IN-3 相关产品
| 产品描述 | 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. |
| 体外活性 | Cholesterol 24-hydroxylase-IN-3 (Compound 4L) (10 μM, 1 h) 对 CH24H 具有选择性抑制作用,对其它 CYP 酶的抑制率较低,其中 CYP3A4、CYP2C8、CYP2C9 和 CYP2D6 的抑制率分别为 7.3%、10%、8.5% 和 49%。 |
| 体内活性 | 胆固醇24-羟化酶-IN-3 (Compound 4L) (30 mg/kg, i.g, 单剂量) 在小鼠体内能够有效通过血脑屏障,并降低脑内24S-羟基胆固醇 (24HC) 的水平,为神经疾病提供了新的治疗策略。 |
| 分子量 | 297.23 |
| 分子式 | C13H10F3N3O2 |
| CAS No. | 1630746-27-8 |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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