1. Immunology/Inflammation
  2. CD38
  3. CVN14

CVN14 是一种高效、选择性且可穿透血脑屏障的 CD38 抑制剂,对人源 IC50 为 19 nM,对小鼠源 IC50 为 2.4 nM。CVN14 以非竞争性方式与 CD38 和 ADPR 结合形成复合物,从而抑制 CD38 的酶活性。CVN14 可用于神经退行性疾病的研究。

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CVN14

CVN14 Chemical Structure

CAS No. : 2925663-26-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CVN14 is a potent, selective and brain-penetrant CD38 inhibitor with human IC50 19 nM, mouse IC50 2.4 nM. CVN14 binds uncompetitively to form a complex with CD38 and ADPR, and inhibits CD38 enzymatic activity. CVN14 can be used for the research of neurodegenerative diseases[1].

体外研究
(In Vitro)

CVN14 可强效抑制人源 CD38,其 IC50 为 19 nM;抑制小鼠 CD38 的 IC50 为 2.4 nM[1]
CVN14 可强效抑制 CHO-hCD38 细胞中人类 CD38 的活性,其 IC50 为 19 nM[1]
CVN14 人类 CD38 紧密结合,其解离常数 Kd 为 3.6 nM,解离半衰期长达 143 min[1]
CVN14 具有良好的体外跨 MDR1-MDCK 细胞单层通透性,外排率为 0.90[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route CLplasma Vdss C0 AUC0-∞ T1/2 Cmax Tmax
Mice[1] 1 mg/kg i.v. 5.5 mL/min/kg 0.84 L/kg 5.77 μM 8.15 μM·h 2.32 h / /
Mice[1] 10 mg/kg p.o. / / / 98.5 μM·h 2.53 h 29.6 μM 0.5 h
体内研究
(In Vivo)

CVN14 (10 mg/kg;口服;单剂量) 显示出较高的脑分布,其 Kpuu,brain 值大于 0.3[1]

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

分子量

382.38

Formula

C17H21F3N6O

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
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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.

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CVN14
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HY-181543
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