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Purity: ≥98%
Stiripentol (formerly known as BCX-2600; BCX2600; STP; trade name: Diacomit) is an FDA-approved anticonvulsant drug that inhibits the activity of several cytochromes P450 (P450s). Stiripentol inhibits N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively. In August 2018, FDA approved Stiripentol to treat seizures associated with Dravet syndrome in patients 2 years of age and older taking clobazam.
| ln Vitro |
Stiripentol (STP) is an anticonvulsant drug that can block CYP3A4's (noncompetitively) and CYP2C19's (competitively) N-demethylation of CLB to N-desmethylclobazam (NCLB). The best models to explain the inhibition of CLB demethylation by Stiripentol (STP) are the competitive inhibition model with Ki=0.52 μM for the cDNA-expressing CYP2C19 and the noncompetitive inhibition model with apparent Ki=1.6 μM for the cDNA-expressing CYP3A4. Stiripentol (STP) has a Ki=0.14 μM and competitively inhibits the formation of OH-NCLB from NCLB by cDNA-expressing CYP2C19[1].
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| ln Vivo |
The difference in temperature between BT1 (39.67±1.09°C) and BT2 (41.32±1.05°C) in mice receiving Stiripentol (STP) monotherapy reaches statistical significance (t=3.097, p<0.05). Between Stiripentol (STP) monotherapy and CLB monotherapy, there is a statistically significant difference in BT2 (t=2.615, p<0.05). The difference between BT1 (40.18±0.58°C) and BT2 (43.03±0.49°C) in mice receiving Stiripentol (STP)+CLB combination therapy reaches statistical significance (t=10.44, p<0.01)[2].
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| References |
[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 |
| Molecular Formula |
C₁₄H₁₈O₃
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| Molecular Weight |
234.29
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| CAS # |
49763-96-4
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| Related CAS # |
Stiripentol-d9;1185239-64-8
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| SMILES |
CC(C)(C)C(O)/C=C/C1=CC=C(OCO2)C2=C1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2682 mL | 21.3411 mL | 42.6821 mL | |
| 5 mM | 0.8536 mL | 4.2682 mL | 8.5364 mL | |
| 10 mM | 0.4268 mL | 2.1341 mL | 4.2682 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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