| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
Sipatrigine targets multiple ion channels. It is a voltage-dependent sodium channel (NaV) blocker and also blocks calcium channels. It inhibits glutamate release. It has been shown to block multiple cardiac ion channels, causing triangulation of the ventricular action potential. It also antagonizes the two-pore-domain K+ channel TREK-1. Its neuroprotective activity is attributed to its ability to inhibit these channels and reduce excitotoxicity.
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| ln Vitro |
In vitro, Sipatrigine is a glutamate release inhibitor and voltage-dependent sodium channel blocker. It inhibits neuronal firing. It blocks voltage-gated sodium and calcium channels in a voltage-dependent manner. It is a neuroprotective agent. Its ability to inhibit glutamate release and reduce neuronal excitability makes it a valuable tool for studying neuroprotection and epilepsy. It is an analog of lamotrigine, sharing similar mechanisms of action.
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| ln Vivo |
In vivo, Sipatrigine displays neuroprotective activity in rat models of cerebral ischemia. It has been investigated for the treatment of stroke. It penetrates the central nervous system. It has potential therapeutic applications for major depression and bipolar depression. By blocking sodium and calcium channels and inhibiting glutamate release, it reduces excitotoxic damage. Its effects on TREK-1 channels may contribute to its antidepressant effects.
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| Enzyme Assay |
The in vitro ion channel assay for Sipatrigine involves measuring its inhibition of sodium or calcium currents using patch-clamp electrophysiology. Cells expressing the ion channels are treated with varying concentrations of Sipatrigine (0.01-100 µM). The inhibition of the current is measured, and IC50 values are calculated. Glutamate release can be measured in neuronal cultures using HPLC or enzyme-linked assays. TREK-1 channel antagonism can be assessed using similar electrophysiological techniques.
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| Cell Assay |
In vitro cellular assays for Sipatrigine use neuronal cell lines or primary neurons. Cells are treated with the compound at concentrations of 0.1-100 µM. Cell viability is assessed under conditions of excitotoxicity (e.g., high glutamate). Neuroprotection is measured by assessing cell survival. Calcium influx is measured using fluorescent indicators. These assays help characterize the compound's neuroprotective mechanism.
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| Animal Protocol |
In vivo animal studies for Sipatrigine involve models of cerebral ischemia, such as the middle cerebral artery occlusion (MCAO) model in rats. The compound is administered intravenously or intraperitoneally at doses of 1-30 mg/kg. The infarct volume is measured, and neurological function is assessed. The compound's ability to reduce brain damage is evaluated. These studies established its neuroprotective efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Sipatrigine indicate that it penetrates the central nervous system. It has a molecular weight of 372.68 and a molecular formula of C15H16Cl3N5. The compound should be stored at -20°C for long-term preservation. It is soluble in DMSO. Its half-life and metabolic profile are consistent with its use in research.
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| References |
Gao Z, Milnes JT, Choisy SC, Leach MJ, Hancox JC, James AF. The neuroprotective agent sipatrigine blocks multiple cardiac ion channels and causes triangulation of the ventricular action potential. Clin Exp Pharmacol Physiol. 2005 Dec;32(12):1088-96. PubMed PMID: 16445575.
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| Additional Infomation |
Sipatrigine is a type of pyrimidine compound.
Sipatrigine (619C89) is a neuroprotective agent with the CAS number 130800-90-7. Its molecular formula is C15H16Cl3N5. It is a multiple channels blocker. It has been investigated for stroke. The compound is a research tool and is not for human therapeutic use. |
| Molecular Formula |
C15H16CL3N5
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|---|---|
| Molecular Weight |
372.68004
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| Exact Mass |
371.047
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| CAS # |
130800-90-7
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| PubChem CID |
60803
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| Appearance |
White to off-white solid powder
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| Density |
1.419 g/cm3
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| Boiling Point |
531.1ºC at 760 mmHg
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| Flash Point |
275ºC
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| LogP |
4.021
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
393
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PDOCBJADCWMDGL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H16Cl3N5/c1-22-2-4-23(5-3-22)15-20-8-11(14(19)21-15)10-6-9(16)7-12(17)13(10)18/h6-8H,2-5H2,1H3,(H2,19,20,21)
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| Chemical Name |
2-(4-methylpiperazin-1-yl)-5-(2,3,5-trichlorophenyl)pyrimidin-4-amine
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| Synonyms |
619C 619C-89 BW-619C-89 BW-619C89 619 C 619C 89 BW 619C-89 BW 619C89 619C 619C89 BW619C89
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~50 mg/mL (~134.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.58 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 (5.58 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 (5.58 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 | 2.6833 mL | 13.4163 mL | 26.8327 mL | |
| 5 mM | 0.5367 mL | 2.6833 mL | 5.3665 mL | |
| 10 mM | 0.2683 mL | 1.3416 mL | 2.6833 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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