Stiripentol ( BCX2600 )

产品货号. M18654 CAS No. 49763-96-4

Stiripentol (STP) 是一种抗惊厥药，可抑制 CYP3A4（非竞争性）和 CYP2C19（竞争性）介导的 CLB N-去甲基化为 NCLB，Ki 为 1.59/0.516 μM，IC50 为 1.58/3.29 μM。

纯度: >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

规格	价格/人民币	库存	数量
5MG	￥381	有现货
10MG	￥608	有现货
25MG	￥1239	有现货
50MG	￥1758	有现货
100MG	￥2973	有现货
200MG	￥4398	有现货
500MG	获取报价	有现货
1G	获取报价	有现货

产品询价大包装询价加入购物车

生物学信息

产品名称

Stiripentol
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

Stiripentol (STP) 是一种抗惊厥药，可抑制 CYP3A4（非竞争性）和 CYP2C19（竞争性）介导的 CLB N-去甲基化为 NCLB，Ki 为 1.59/0.516 μM，IC50 为 1.58/3.29 μM。
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.(In Vitro):Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to N-desmethylclobazam (NCLB) mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively). 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.(In Vivo):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).
体外实验

Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to N-desmethylclobazam (NCLB) mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively). 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.
体内实验

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).
同义词

BCX2600
通路

Others
靶点

Other Targets
受体

CYP3A4| CYP2C19
研究领域

——
适应症

——

化学信息

CAS Number

49763-96-4
分子量

234.29
分子式

C14H18O3
纯度

>98% (HPLC)
溶解度

DMSO : 150 mg/mL 640.23 mM;
SMILES

CC(C)(C)C(O)\C=C\c1ccc2OCOc2c1
化学全称

——

运输与储存

储存条件

(-20℃)
运输条件

With Ice Pack
稳定性

≥ 2 years

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.

计算器

浓度计算器

摩尔计算器

分子量计算器

产品手册