ALE-0540
Based on 1 Customer Validation
ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC50 values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the study of pain.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.35%
- CAS. Nr.: 234779-34-1
- Formel: C14H11N3O5
- Molecular Weight:301.25
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 5.88 μM (the binding of NGF to tyrosine kinase (Trk) A and TrkA); 3.72 μM (the binding of NGF to p75 and TrkA)[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-12 | EC50 |
22 μM
Compound: 1; ALE-0540
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Inhibition of NGF-induced TrkA auto-phosphorylation in rat PC12 cells incubated for 15 mins by chemiluminescence based method
Inhibition of NGF-induced TrkA auto-phosphorylation in rat PC12 cells incubated for 15 mins by chemiluminescence based method
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[PMID: 27779399] |
| PC-12 | IC50 |
3.72 μM
Compound: 1
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Competitive binding against Nerve growth factor to p75-NGF receptor in PC12 cells
Competitive binding against Nerve growth factor to p75-NGF receptor in PC12 cells
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[PMID: 11931608] |
| PC-12 | IC50 |
3.72 μM
Compound: 1
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Inhibition of NGF-stimulated Trk A in PC12 cells
Inhibition of NGF-stimulated Trk A in PC12 cells
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[PMID: 11931608] |
| PC-12 | IC50 |
5.88 μM
Compound: 1; ALE-0540
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Inhibition of binding of [125I]-NGF to TrkA in rat PC12 cells incubated for 2 hrs by gamma counting method
Inhibition of binding of [125I]-NGF to TrkA in rat PC12 cells incubated for 2 hrs by gamma counting method
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[PMID: 27779399] |
Chemical Information
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CAS. Nr. 234779-34-1
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Appearance Solid
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Molecular Weight 301.25
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Formel C14H11N3O5
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Color Light yellow to yellow
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SMILES
O=C1N(NCCO)C(C2=CC([N+]([O-])=O)=CC3=CC=CC1=C23)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 125 mg/mL (414.94 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, 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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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PC12 NGF-Induced Neuronal Differentiation Culture
PC12 cells are a rat adrenal pheochromocytoma clonal line that responds to NGF by stopping proliferation and extending branching neurite-like processes; after longer NGF exposure, cells develop long processes and neuronal-like ultrastructural and functional features. NGF-induced differentiation is read out mainly by neurite outgrowth, reduced proliferation, microtubule assembly, and neuronal differentiation-associated proteins such as MAPs, tau, GAP-43, and synapsin-1.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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PC12 NGF-induced neuronal-like differentiation
PC12 cells are a rat adrenal pheochromocytoma-derived clonal cell line that responds to nerve growth factor by stopping proliferation and extending neurites, producing a sympathetic neuron-like phenotype used to study neuronal differentiation and neurite outgrowth. NGF acts through TrkA-dependent signaling, and neurite outgrowth is associated with ERK/Akt signaling, microtubule organization, neuronal-marker expression, and increased electrophysiological neuronal features such as sodium-channel density. The main assay readout is morphological differentiation, usually measured as the percentage of neurite-bearing cells, neurite length, neurite number, or total neurite length per cell. Additional readouts include GAP-43, tyrosine hydroxylase, βIII-tubulin, neurofilament, synapsin I, synaptophysin, ERK phosphorylation, Akt phosphorylation, and sodium-channel current density.
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (759 KB)
- English - EN (759 KB)
- Français - FR (759 KB)
- Deutsch - DE (759 KB)
- Norwegian - NO (759 KB)
- Español - ES (759 KB)
- Swedish - SV (759 KB)
- Italian - IT (759 KB)
- Korean - KR (759 KB)
- Portuguese - PT (759 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3195 mL | 16.5975 mL | 33.1950 mL | 82.9876 mL |
| 5 mM | 0.6639 mL | 3.3195 mL | 6.6390 mL | 16.5975 mL | |
| 10 mM | 0.3320 mL | 1.6598 mL | 3.3195 mL | 8.2988 mL | |
| 15 mM | 0.2213 mL | 1.1065 mL | 2.2130 mL | 5.5325 mL | |
| 20 mM | 0.1660 mL | 0.8299 mL | 1.6598 mL | 4.1494 mL | |
| 25 mM | 0.1328 mL | 0.6639 mL | 1.3278 mL | 3.3195 mL | |
| 30 mM | 0.1107 mL | 0.5533 mL | 1.1065 mL | 2.7663 mL | |
| 40 mM | 0.0830 mL | 0.4149 mL | 0.8299 mL | 2.0747 mL | |
| 50 mM | 0.0664 mL | 0.3320 mL | 0.6639 mL | 1.6598 mL | |
| 60 mM | 0.0553 mL | 0.2766 mL | 0.5533 mL | 1.3831 mL | |
| 80 mM | 0.0415 mL | 0.2075 mL | 0.4149 mL | 1.0373 mL | |
| 100 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8299 mL |
ALE-0540 Related Classifications
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