LY367385
Based on 3 publication(s) in Google Scholar
LY367385 is a highly selective and potent mGluR1a antagonist. LY367385 has an IC50 of 8.8 μM for inhibiting of quisqualate-induced phosphoinositide (PI) hydrolysis, compared with >100 μM for mGlu5a. LY367385 has neuroprotective, anticonvulsant and antiepileptic effects.
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- 純度: 99.0%
- CAS 番号: 198419-91-9
- 分子式: C10H11NO4
- 分子量:209.20
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 LY367385
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生物活性
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mGluR1a 8.8 μM (IC50) |
LY367385 combined with N-methyl-D-aspartate (NMDA) during the toxic pulse attenuates neuronal degeneration in a concentration-dependent fashion, with a maximal reduction of NMDA toxicity ranging from 40 to 60%. LY367385 shows greater efficacy than LY367366 and neither of these compounds influenced neuronal viability per se. LY367385 shows potent neuroprotective effects, with causing a 50% reduction in (S)-3,5-Dihydroxyphenylglycine (DHPG) potentiation at a concentration of 10 nM. Under experimental conditions at higher concentrations of antagonist, LY367385 a completely antagonized the amplification of NMDA toxicity by DHPG[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In genetically epilepsy prone rats, LY367385 reduces sound-induced clonic seizures. LY367385, 160 nM bilaterally, fully suppresses clonic seizures after 2-4 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 198419-91-9
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性状 Solid
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分子量 209.20
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分子式 C10H11NO4
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Color White to off-white
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SMILES
OC([C@H](C1=C(C=C(C(O)=O)C=C1)C)N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Preso enhances mGluR1-mediated excitotoxicity by modulating the phosphorylation of mGluR1-Homer1 complex and facilitating an ER stress after traumatic brain injury. [Abstract]2024 Mar 26;10(1):153. PMID: 38531909 -
Brain Behav Immun
NR2B-CaMKII signaling in the dentate gyrus driven by astrocytic P2Y1Rs mediates the antidepressant effect of low-dose LPS. [Abstract]2026 Jul:135:106529. PMID: 41796645 -
Neurochem Int
Red nucleus mGluR1 and mGluR5 facilitate the development of neuropathic pain through stimulating the expressions of TNF-α and IL-1β. [Abstract]2024 Sep:178:105786. PMID: 38843952
溶剤 & 溶解度
H2O : 10 mg/mL (47.80 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[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 and mGlu5 receptors. Neuropharmacology. 1999 Feb;38(2):199-207. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.7801 mL | 23.9006 mL | 47.8011 mL | 119.5029 mL |
| 5 mM | 0.9560 mL | 4.7801 mL | 9.5602 mL | 23.9006 mL | |
| 10 mM | 0.4780 mL | 2.3901 mL | 4.7801 mL | 11.9503 mL | |
| 15 mM | 0.3187 mL | 1.5934 mL | 3.1867 mL | 7.9669 mL | |
| 20 mM | 0.2390 mL | 1.1950 mL | 2.3901 mL | 5.9751 mL | |
| 25 mM | 0.1912 mL | 0.9560 mL | 1.9120 mL | 4.7801 mL | |
| 30 mM | 0.1593 mL | 0.7967 mL | 1.5934 mL | 3.9834 mL | |
| 40 mM | 0.1195 mL | 0.5975 mL | 1.1950 mL | 2.9876 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
LY367385 関連分類
HY-107515 関連分類
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