LE 300
Based on 2 publication(s) in Google Scholar
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.5%
- CAS 番号: 274694-98-3
- 分子式: C20H22N2
- 分子量:290.40
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 LE 300
MoreDopamine Receptor アイソフォーム固有の製品をすべて表示
More5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Human D1 Receptor 1.9 nM (Ki) |
5-HT2A Receptor |
Human D5 Receptor 7.5 nM (Ki) |
Rat 5-HT2A 8.32 (pA2) |
化学情報
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CAS 番号 274694-98-3
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性状 Solid
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分子量 290.40
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分子式 C20H22N2
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Color Off-white to light yellow
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SMILES
CN1CCC2=C(NC3=C2C=CC=C3)CC4=CC=CC=C4CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Neuron
2024 Jul 25:S0896-6273(24)00494-X. PMID: 39094559 -
Biomed Pharmacother
Polypharmacological profiling across protein target families and cellular pathways using the multiplexed cell-based assay platform safetyProfiler reveals efficacy, potency and side effects of drugs. [Abstract]2024 Nov:180:117523. PMID: 39405910
溶剤 & 溶解度
DMSO : 29.04 mg/mL (100.00 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kassack MU, et al. Pharmacological characterization of the benz[d]indolo[2,3-g]azecine LE300, a novel type of a nanomolar dopamine receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol. 2002 Dec;366(6):543-50. [Content Brief]
[2]. Rostom SA. Novel fused pyrrole heterocyclic ring systems as structure analogs of LE 300: Synthesis and pharmacological evaluation as serotonin 5-HT(2A), dopamine and histamine H(1) receptor ligands. Arch Pharm (Weinheim). 2010 Feb;343(2):73-80. [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 (protect from light, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4435 mL | 17.2176 mL | 34.4353 mL | 86.0882 mL |
| 5 mM | 0.6887 mL | 3.4435 mL | 6.8871 mL | 17.2176 mL | |
| 10 mM | 0.3444 mL | 1.7218 mL | 3.4435 mL | 8.6088 mL | |
| 15 mM | 0.2296 mL | 1.1478 mL | 2.2957 mL | 5.7392 mL | |
| 20 mM | 0.1722 mL | 0.8609 mL | 1.7218 mL | 4.3044 mL | |
| 25 mM | 0.1377 mL | 0.6887 mL | 1.3774 mL | 3.4435 mL | |
| 30 mM | 0.1148 mL | 0.5739 mL | 1.1478 mL | 2.8696 mL | |
| 40 mM | 0.0861 mL | 0.4304 mL | 0.8609 mL | 2.1522 mL | |
| 50 mM | 0.0689 mL | 0.3444 mL | 0.6887 mL | 1.7218 mL | |
| 60 mM | 0.0574 mL | 0.2870 mL | 0.5739 mL | 1.4348 mL | |
| 80 mM | 0.0430 mL | 0.2152 mL | 0.4304 mL | 1.0761 mL |