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Stiripentol

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Purity:99.93%

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COA HNMR HPLC LCMS

Stiripentol

Catalog No. T4498Cas No. 49763-96-4

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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Pack Size	Price	Availability
5 mg	$47	In Stock
10 mg	$75	In Stock
25 mg	$153	In Stock
50 mg	$217	In Stock
100 mg	$367	In Stock
200 mg	$543	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock

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Product Introduction

Bioactivity

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	CYP2C19:3.29 μM, CYP3A4:1.58 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 treated with Stiripentol (STP) monotherapy, the difference between BT1 (39.67±1.09°C) and BT2 (41.32±1.05°C) is statistically significant (t=3.097, p<0.05). The difference in BT2 between Stiripentol (STP) monotherapy and CLB monotherapy is also statistically significant (t=2.615, p<0.05). In mice treated with Stiripentol (STP)+CLB combination therapy, the difference between BT1 (40.18±0.58°C) and BT2 (43.03±0.49°C) is statistically significant (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].
Alias	BCX2600, Diacomit

Chemical Properties

Molecular Weight	234.29
Formula	C14H18O3
Cas No.	49763-96-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

H2O: 5 mg/mL

DMSO: 55 mg/mL (234.75 mM)

Ethanol: 30 mg/mL

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.2682 mL	21.3411 mL	42.6821 mL	213.4107 mL
5 mM	0.8536 mL	4.2682 mL	8.5364 mL	42.6821 mL
10 mM	0.4268 mL	2.1341 mL	4.2682 mL	21.3411 mL
20 mM	0.2134 mL	1.0671 mL	2.1341 mL	10.6705 mL
50 mM	0.0854 mL	0.4268 mL	0.8536 mL	4.2682 mL
100 mM	0.0427 mL	0.2134 mL	0.4268 mL	2.1341 mL

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