Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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LY2365109 (LY-2365109) is a novel and potent glycine transporter 1 (GlyT1) inhibitor (IC50 = 15.8 nM) with the potential to be used as an antiictogenic drug.
ln Vivo |
Glycine levels in cerebrospinal fluid rise in a dose-dependent manner when oral LY2365109 hydrochloride (0.3–30 mg/kg) is administered [1]. In mice, the threshold for seizures is raised by LY2365109 hydrochloride [2].
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Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (250-300 g) [1]
Doses: 0.3 mg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg, 30 mg/kg Route of Administration: Oral Experimental Results: Produces a dose-dependent increase in cerebrospinal fluid glycine levels measured 1 hour after administration. |
References |
[1]. Perry KW et al. Neurochemical and behavioral profiling of the selective GlyT1 inhibitors ALX5407 and LY2365109 indicate a preferential action in caudal vs. cortical brain areas. Neuropharmacology. 2008 Oct;55(5):743-54.
[2]. Shen HY et al. Glycine transporter 1 is a target for the treatment of epilepsy. Neuropharmacology. 2015 Dec;99:554-65. |
Molecular Formula |
C22H28CLNO5
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Molecular Weight |
421.91
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CAS # |
1779796-27-8
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Related CAS # |
1779796-27-8 (HCl);868265-28-5;
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SMILES |
O=C(O)CN(CCOC1=CC=C(C2=CC=C(OCO3)C3=C2)C=C1C(C)(C)C)C.[H]Cl
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Synonyms |
LY-2365109 LY 2365109 LY2365109
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 : ≥ 31 mg/mL (~73.48 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.93 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 25.0 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: ≥ 2.5 mg/mL (5.93 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 25.0 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: ≥ 2.5 mg/mL (5.93 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 | 2.3702 mL | 11.8509 mL | 23.7017 mL | |
5 mM | 0.4740 mL | 2.3702 mL | 4.7403 mL | |
10 mM | 0.2370 mL | 1.1851 mL | 2.3702 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.