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Purity: ≥98%
Eliprodil (formerly known as SL-820715) is a non-competitive NR2B-NMDA receptor antagonist with IC50 value of 1 uM, it is less potent for NR2A- and NR2C-containing receptors with IC50 > 100 uM. NMDA receptors play a key role in mediating glutamate-induced excitotoxicity, thus it is believed that NMDA antagonists would be neuroprotective after a stroke or other traumatic brain injury. Eliprodil protects pyramidal neurons in hippocampal slices from hypoxic or ischemic damage. Eliprodil also stimulates CNS myelination and may have potential for multiple sclerosis.
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| Additional Infomation |
Eliprodil is a racemate comprising equimolar amounts of (R)- and (S)-eliprodil. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and an anti-ischaemic agent that exhibits neuroprotective properties. It has a role as a geroprotector, a NMDA receptor antagonist, a neuroprotective agent and a calcium channel blocker. It contains a (R)-eliprodil and a (S)-eliprodil.
Eliprodil has been used in trials studying the treatment of Parkinson Disease and Movement Disorders. |
| Molecular Formula |
C₂₀H₂₃CLFNO
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| Molecular Weight |
347.85
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| Exact Mass |
347.145
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| CAS # |
119431-25-3
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| Related CAS # |
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| PubChem CID |
60703
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| Appearance |
White to off-white solid powder
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| Density |
1.205 g/cm3
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| Boiling Point |
474.1ºC at 760 mmHg
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| Flash Point |
240.5ºC
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| Vapour Pressure |
8.57E-10mmHg at 25°C
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| Index of Refraction |
1.58
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| LogP |
4.405
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
359
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GGUSQTSTQSHJAH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2
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| Chemical Name |
1-(4-chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
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| Synonyms |
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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 |
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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: 1.43 mg/mL (4.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 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: ≥ 1.43 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8748 mL | 14.3740 mL | 28.7480 mL | |
| 5 mM | 0.5750 mL | 2.8748 mL | 5.7496 mL | |
| 10 mM | 0.2875 mL | 1.4374 mL | 2.8748 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.
 Effect of eliprodil on the APD (APD90) in canine right ventricular papillary muscle.Br J Pharmacol.2004 Sep;143(1):152-8 |
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 Effect of eliprodil on the APD (APD90) in the presence ofIK1block by BaCl2(10μm) in canine right ventricular papillary muscle.Br J Pharmacol.2004 Sep;143(1):152-8 |
(a) Effect of 1μmeliprodil on QTcinterval of the volume-conducted ECG recorded in isolated Langendorff-perfused rabbit heart in the absence and presence of 10μmBaCl2(b) The percentage change of the eliprodil-evoked QTclengthening in normal and in attenuated repolarisation reserve preparations.Br J Pharmacol.2004 Sep;143(1):152-8 |
Proarrhythmic effect of 1μmeliprodil after the administration of 10μmBaCl2on volume-conducted ECG recorded in isolated Langendorff-perfused rabbit heart.Br J Pharmacol.2004 Sep;143(1):152-8 |
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 Lack of effect of 1μmeliprodil in canine ventricular myocytes on the inward rectifier potassium current (IK1) measured as the steady-state current at the end of the test pulse in the voltage range between −80 to 0 mV (a), on the transient outward current (Ito) (b) and on the slow component of the delayed rectifier potassium current (IKs).Br J Pharmacol.2004 Sep;143(1):152-8 |
 Effect of 1μmeliprodil on the rapid component of the delayed rectifier potassium current (IKr) in canine ventricular myocytes. (Left panel) Original current traces under control conditions and after application of 1μmeliprodil. (Right panel) The current–voltage relationship ofIKrunder control conditions and in the presence of 1μmeliprodil (mean±s.e.m.).Br J Pharmacol.2004 Sep;143(1):152-8 |
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