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1mg |
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LY367385 (LY-367385) is a novel and potent mGlu1a receptor antagonist (IC50 = 8.8 μM) with neuroprotective, anticonvulsant and antiepileptic effects. It inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.
Targets |
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ln Vitro |
LY367385 coupled with N-methyl-D-aspartate (NMDA) during the toxic pulse reduces neuronal degeneration in a concentration-dependent manner, with a maximum decrease of NMDA toxicity of 40 to 60%. LY367385 is more effective than LY367366, and neither chemical has an effect on neuronal viability in general. LY367385 has strong neuroprotective properties, causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a dose of 10 nM. Under experimental conditions, at greater antagonist doses, LY367385 totally inhibited the amplification of NMDA toxicity by DHPG[2].
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ln Vivo |
Intracerebroventricular (icv) administration of LY367385 has been observed in DBA/2 and lh/lh lethargic mice, as well as targeted administration of LY367385 into the inferior colliculus of genetically epilepsy-prone rats (GEPR). LY367385 quickly and temporarily suppresses sound-induced clonic convulsions in DBA/2 mice (ED50 = 12 nM, icv, 5 min). When LY367385, 250 nM, is administered to sluggish mice, the occurrence of spontaneous spike and wave discharges on the electroencephalogram is dramatically reduced[3]. This effect lasts for 30 to more than 150 minutes. In rats predisposed to epilepsy genetically, LY367385 lessens clonic seizures brought on by sound. After 2-4 hours, LY367385, 160 nM bilaterally, completely inhibits clonic seizures[3].
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References |
[1]. Clark et al. (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. November 1997, 7 (21): 2777-2780.
[2]. Bruno V, et al. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a [3]. Chapman AG, et al. Anticonvulsant actions of LY 367385 ((+)-2-methyl-4-carboxyphenylglycine) and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur J Pharmacol. 1999 Feb 26;368(1):17-24. |
Molecular Formula |
C10H11NO4
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Molecular Weight |
209.2
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Exact Mass |
209.0688
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CAS # |
198419-91-9
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Related CAS # |
LY367385 hydrochloride;2829282-00-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
OC(C1C=CC([C@@H](C(=O)O)N)=C(C)C=1)=O
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Synonyms |
LY-367385 LY 367385 LY367385
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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 |
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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.7801 mL | 23.9006 mL | 47.8011 mL | |
5 mM | 0.9560 mL | 4.7801 mL | 9.5602 mL | |
10 mM | 0.4780 mL | 2.3901 mL | 4.7801 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.