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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.5%
- CAS. Nr.: 274694-98-3
- Formel: C20H22N2
- Molecular Weight:290.40
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Speicherung:
-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 Citing Use of MedChemExpress (MCE) LE 300
MoreAlle Dopamine Receptor Isoform-spezifische Produkte anzeigen
MoreAlle 5-HT Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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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) |
Chemical Information
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CAS. Nr. 274694-98-3
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Appearance Solid
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Molecular Weight 290.40
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-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
Lösungsmittel & Löslichkeit
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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 |