Stiripentol

产品编号: T4498 别名:

斯利潘托,Diacomit,BCX2600

Stiripentol 是抗惊厥剂，对 CYP3A4 (非竞争性) 及 CYP2C19 (竞争性地) 介导的 CLB 向 N-desmethylclobazam (NCLB) 的 N-去甲基化具有抑制作用。

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CAS：49763-96-4

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59/0.516 μM and IC50 of 1.58/3.29 μM, respectively.

体外活性

The inhibition of CLB demethylation by Stiripentol (STP) is best described by a noncompetitive inhibition model with apparent Ki (1.6 μM) for the cDNA-expressing CYP3A4 and by a competitive inhibition model with Ki (0.52 μM) for the cDNA-expressing CYP2C19. Formation of OH-NCLB from NCLB by cDNA-expressing CYP2C19 is competitively inhibited by Stiripentol (STP) with a Ki: 0.14 μM [1].

体内活性

In mice treating with Stiripentol (STP) monotherapy, the difference between BT1 (39.67±1.09°C) and BT2 (41.32±1.05°C) reaches statistical significance (t=3.097, p<0.05). The difference in BT2 between Stiripentol (STP) monotherapy and CLB monotherapy is statistically significant (t=2.615, p<0.05). In mice treating with Stiripentol (STP)+CLB combination therapy, the difference between BT1 (40.18±0.58°C) and BT2 (43.03±0.49°C) reaches statistical significance (t=10.44, p<0.01)[2].

细胞实验

The inhibition constants (apparent Ki) of Stiripentol (STP) for CLB demethylation by CYP3A4 and CYP2C19 are determined using various concentrations of CLB (2, 10, 20, 40, 60, and 100 μM) with increasing concentrations of Stiripentol (STP) (0, 0.5, 1, 2, and 5 μM). Concerning NCLB hydroxylation by CYP2C19, the apparent Ki is similarly determined with different concentrations of NCLB (1.5, 4, 6, 8, 12, and 14 μM) and STP (0, 0.1, 0.5, 1, and 2 μM). IC50 values are determined by coincubation of the substrate at the concentration in the range of the therapeutic plasma concentrations (2 μM CLB or 14 μM NCLB) with increasing concentrations of Stiripentol (STP) (0.001-10 μM) [1].

动物实验

Two age groups, p1M (n=18, age 4 weeks) and p5M (n=18, age 5-10 months), of Scn1aRX/+ mice are assigned in this experiment. Both groups are divided randomly into three subgroups (n=6), and each subgroup is administered Stiripentol (STP) (300 mg/kg) alone, CLB (6.62 mg/kg) alone, or a combination of Stiripentol (STP) (p1M; 150 mg/kg, p5M; 300 mg/kg) and CLB (6.62 mg/kg). All drugs are administered by intraperitoneal injection (i.p.) after a 48-h recovery from baseline seizure study. Blood samples are collected at 1 h and 20 min after administration of CLB or STP+CLB for measurement of plasma concentrations of CLB and N-desmethylclobazam, respectively [2].

Cas No.

49763-96-4

分子式

C14H18O3

分子量

234.295

别名

斯利潘托;Diacomit;BCX2600;Stiripentol

参考文献

[1]Giraud C, et al. In vitro and in vivo inhibitory effect of stiripentol on clobazam metabolism.Drug Metab Dispos. 2006 Apr;34(4):608-11. Epub 2006 Jan 13.[2]Cao D, et al. Efficacy of stiripentol in hyperthermia-induced seizures in a mouse model of Dravet syndrome. Epilepsia. 2012 Jul;53(7):1140-5.

引用文献

[1]Avdeef A, Kansy M. Predicting Solubility of Newly-Approved Drugs (2016–2020) with a Simple ABSOLV and GSE (Flexible-Acceptor) Consensus Model Outperforming Random Forest Regression. Journal of Solution Chemistry. 2022: 1-36.

储存和溶解度

H2O:5 mg/mL
DMSO:50 mg/mL
Ethanol:30 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Stiripentol 49763-96-4

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要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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Keywords

Stiripentol 斯利潘托 Inhibitor BCX-2600 Diacomit BCX 2600 inhibit CYPs BCX2600 Cytochrome P450 49763-96-4

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