2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. hCYP3A4-IN-1

hCYP3A4-IN-1 (compound C6) 是一种口服有效的 hCYP3A4 抑制剂。 hCYP3A4-IN-1 在人肝微粒体 (HLM) 和 CHO-3A4 稳定转染细胞系中对 hCYP3A4 的 IC50 值分别为 43.93 nM 和 153.00 nM。 hCYP3A4-IN-1 以竞争性方式有效抑制 CYP3A4 催化的 N-乙基-1,8-萘二甲酰亚胺 (NEN) 羟基化 (Ki = 30.00 nM)。

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hCYP3A4-IN-1 Chemical Structure

hCYP3A4-IN-1 Chemical Structure

CAS No. : 3003751-14-9

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hCYP3A4-IN-1 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
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

hCYP3A4-IN-1 (compound C6) is a potent, orally active hCYP3A4 inhibitor. hCYP3A4-IN-1 shows the IC50 values of 43.93 nM and 153.00 nM against hCYP3A4 in human liver microsomes (HLMs) and CHO-3A4 stably transfected cell line, respectively. hCYP3A4-IN-1 potently inhibits CYP3A4-catalyzed N-ethyl-1,8-naphthalimide (NEN) hydroxylation in a competitive manner (Ki = 30.00 nM)[1].

IC50 & Target

CYP3A4

43.93 nM (IC50)

体内研究
(In Vivo)

hCYP3A4-IN-1 (compound C6) 在 HLM 中表现出适当的代谢稳定性，并在小鼠中表现出良好的安全性[1]。
hCYP3A4-IN-1 (100 mg/kg，口服给药，一次)显著增加 midazolam（灌胃，10 mg/kg）的 AUC(0-inf) 3.63 倍，并强烈延长其小鼠体内的半衰期，是溶剂组的 1.66 倍[1]。
Pharmacokinetic Parameters of hCYP3A4-IN-1 in mice[1].

CMC-Na + Midazolam C6 (25 mg/kg) + Midazolam C6 (100 mg/kg) + Midazolam
Tmax (min) 8.00 ± 2.74 5.83 ± 2.04 10.00 ± 0.00
Cmax (ng/mL) 194.20 ± 138.88 312.00 ± 141.40 494.67 ± 210.22
AUC0-24 (ng/mL∗min) 7520.83 ± 2413.78 14784.92 ± 3501.33 27330.95 ± 6664.85
t1/2 (min) 36.33 ± 14.46 54.96 ± 20.87 60.37 ± 27.67

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

302.37

Formula

C20H18N2O
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

hCYP3A4-IN-1 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:

hCYP3A4-IN-13003751-14-9Cytochrome P450CYPsCHO-3A4liver microsomesorally activeInhibitorinhibitorinhibit

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