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Stiripentol

Catalog No. T4498   CAS 49763-96-4
Synonyms: BCX2600, Diacomit

Stiripentol (BCX2600) (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.

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Stiripentol Chemical Structure
Stiripentol, CAS 49763-96-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 75.00
25 mg In stock $ 153.00
50 mg In stock $ 217.00
100 mg In stock $ 367.00
200 mg In stock $ 543.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.93%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Stiripentol (BCX2600) (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.
Targets&IC50 CYP3A4:1.58 μM, CYP2C19:3.29 μM
In vitro 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].
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)[2].
Cell Research 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].
Animal Research 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].
Synonyms BCX2600, Diacomit
Molecular Weight 234.29
Formula C14H18O3
CAS No. 49763-96-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 5 mg/mL

DMSO: 55 mg/mL (234.75 mM)

Ethanol: 30 mg/mL

TargetMolReferences and Literature

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.

TargetMolCitations

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Metabolism Compound Library Anti-Metabolism Disease Compound Library Approved Drug Library NO PAINS Compound Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Compound Library

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Keywords

Stiripentol 49763-96-4 Metabolism P450 Inhibitor BCX2600 inhibit BCX 2600 CYPs Diacomit BCX-2600 Cytochrome P450 inhibitor

 

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