LY 344864
Based on 2 publication(s) in Google Scholar
LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.
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- Pureza : 98.59%
- No. CAS: 186544-26-3
- Fòrmula: C21H22FN3O
- Peso molecular:351.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) LY 344864
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
human 5-HT1F Receptor 0.006 μM (Ki) |
5-HT1F Receptor |
human 5-HT1A Receptor 0.530 μM (Ki) |
human 5-HT1B Receptor 0.549 μM (Ki) |
human 5-HT1D Receptor 0.575 μM (Ki) |
human 5-HT1E Receptor 1.415 μM (Ki) |
human 5-HT2B Receptor 1.695 μM (Ki) |
Human 5-HT2A Receptor 3.499 μM (Ki) |
Human 5-HT3A Receptor 3.935 mM (Ki) |
Human 5-HT7 Receptor 4.851 μM (Ki) |
rat α2-adrenergic receptor 3.69 μM (Ki) |
rat α1-adrenergic receptor 5.06 μM (Ki) |
In Vitro
LY 344864 binds to human 5-HT1F, 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT3A, 5-HT2B, 5-HT2C, 5-HT7, rat α1-adrenergic, rat α2-adrenergic receptors with Kis of 0.006, 0.530, 0.549, 0.575, 1.415, 3.935, 1.695, 3.499, 4.851, 5.06 and 3.69 μM, respectively[1].
LY 344864 is a inducer of mitochondrial biogenesis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
LY 344864 (1 mg/kg; i.v.; once) can cross the blood brain barrier to some extent in rats[1].
LY 344864 (2 mg/kg; i.p.; daily for 14 days) attenuates dopaminergic neuron loss and improved behavioral endpoints in a Parkinson’s disease mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats, migraine pain model[1]
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Dosage:1-10 ng/kg (oral), 0.3-2 ng/kg (intravenous)
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Administration:Oral, 75 minutes before trigeminal stimulation or intravenous, 10 minutes before trigeminal stimulation
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Result:When given intravenously 10 minutes before stimulation, inhibited inflammation with an ID50 (median infective dose) of 0.6 ng/kg. When administered orally 75 minutes before trigeminal stimulation, an ID50 of 1.2 ng/kg was obtained.
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Animal Model:Male C57BL/6 mice, Parkinson’s disease model[2]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection, daily for 14d beginning 7d post-lesion
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Result:Attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals, also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect.
Chemical Information
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No. CAS 186544-26-3
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Appearance Solid
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Peso molecular 351.42
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Fòrmula C21H22FN3O
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Color White to off-white
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SMILES
O=C(NC1=CC2=C(NC3=C2C[C@H](N(C)C)CC3)C=C1)C4=CC=C(F)C=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (284.56 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Phebus LA, Johnson KW, Zgombick JM, Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brainpenetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. [Content Brief]
[2]. Scholpa NE, et al. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol. 2018 Jan;175(2):348-358. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8456 mL | 14.2280 mL | 28.4560 mL | 71.1399 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | 14.2280 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL | 7.1140 mL | |
| 15 mM | 0.1897 mL | 0.9485 mL | 1.8971 mL | 4.7427 mL | |
| 20 mM | 0.1423 mL | 0.7114 mL | 1.4228 mL | 3.5570 mL | |
| 25 mM | 0.1138 mL | 0.5691 mL | 1.1382 mL | 2.8456 mL | |
| 30 mM | 0.0949 mL | 0.4743 mL | 0.9485 mL | 2.3713 mL | |
| 40 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7785 mL | |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5691 mL | 1.4228 mL | |
| 60 mM | 0.0474 mL | 0.2371 mL | 0.4743 mL | 1.1857 mL | |
| 80 mM | 0.0356 mL | 0.1778 mL | 0.3557 mL | 0.8892 mL | |
| 100 mM | 0.0285 mL | 0.1423 mL | 0.2846 mL | 0.7114 mL |
LY 344864 Related Classifications
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