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TP0472993 {[allProObj[0].p_purity_real_show]}

货号:A1721473

TP0472993是一种口服有效的细胞色素 P450 (CYP) 4A11 和 CYP4F2 的双抑制剂,IC50 值分别为 140 nM 和 40 nM,适用于肾脏疾病的研究。

TP0472993 化学结构 CAS号:2126874-77-7
TP0472993 化学结构
CAS号:2126874-77-7
TP0472993 3D分子结构
CAS号:2126874-77-7
TP0472993 化学结构 CAS号:2126874-77-7
TP0472993 3D分子结构 CAS号:2126874-77-7
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TP0472993 纯度/质量文件 产品仅供科研

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TP0472993 生物活性

描述 CYP4A11/CYP4F2-IN-2 acts as a potent, orally available inhibitor that targets both cytochrome P450 4A11 and CYP4F2 enzymes, displaying IC50 values of 140 nM and 40 nM, respectively. This dual inhibitor holds promise for studies related to kidney diseases[1].
体内研究

Administered orally in a single dose ranging from 0.03 to 1 mg/kg, CYP4A11/CYP4F2-IN-2 proportionally decreases the production of 20-HETE in the kidneys of rats[1].

When given intravenously at 0.5 mg/kg to mice, CYP4A11/CYP4F2-IN-2 shows a low clearance rate (1430 mL/h/kg), a moderate volume of distribution at steady state (763 mL/kg), and a short half-life (0.424 hours)[1].

At a dosage of 1 mg/kg administered intravenously to Sprague-Dawley (SD) rats, the inhibitor demonstrates a low clearance rate (226 mL/h/kg), a moderate volume of distribution at steady state (839 mL/kg), and a half-life of approximately 3.01 hours[1].

Following oral administration at 1 mg/kg to SD rats, CYP4A11/CYP4F2-IN-2 reaches a maximum concentration (Cmax) of 623 ng/mL, has a half-life of 3.03 hours, and exhibits high bioavailability (97.7%)[1].

体外研究

CYP4A11/CYP4F2-IN-2 effectively reduces the production of 20-Hydroxyeicosatetraenoic acid (20-HETE) from arachidonic acid within human kidney microsomes, showing an IC50 value of 29 nM[1].

TP0472993 参考文献

[1]Kawamura M, et, al. Discovery of Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition. J Med Chem. 2022 Nov 10;65(21):14599-14613.

[2]Wunder F, et al. Characterization of the cellular activity of PDE 4 inhibitors using two novel PDE 4 reporter celllines. Mol Pharm. 2013 Oct 7;10(10):3697-705.

TP0472993 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.65mL

3.33mL

1.66mL

33.29mL

6.66mL

3.33mL

TP0472993 技术信息

CAS号2126874-77-7
分子式C16H20N4O2
分子量 300.356
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 25 mg/mL(83.23 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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