1. Neuronal Signaling Protein Tyrosine Kinase/RTK
  2. Trk Receptor
  3. ALE-0540

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.

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ALE-0540

ALE-0540 Chemical Structure

CAS No. : 234779-34-1

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5 mg En stock
10 mg En stock
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100 mg   Obtenir un devis  

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Description

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[1].

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
Cell Line Type Value Description References
PC-12 EC50
22 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
PC-12 EC50
22 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
PC-12 EC50
22 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
PC-12 IC50
3.72 3
Compound: 1
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
[PMID: 11931608]
PC-12 IC50
3.72 3
Compound: 1
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
[PMID: 11931608]
PC-12 IC50
5.88 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
PC-12 IC50
3.72 3
Compound: 1
Inhibition of NGF-stimulated Trk A in PC12 cells
Inhibition of NGF-stimulated Trk A in PC12 cells
[PMID: 11931608]
PC-12 IC50
5.88 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
PC-12 IC50
5.88 3
Compound: 1; ALE-0540
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
[PMID: 27779399]
Masse moléculaire

301.25

Formule

C14H11N3O5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(NCCO)C(C2=CC([N+]([O-])=O)=CC3=CC=CC1=C23)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3195 mL 16.5975 mL 33.1950 mL
5 mM 0.6639 mL 3.3195 mL 6.6390 mL
View the 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.

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Pureté et documentation
Références

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nom du produit:
ALE-0540
Cat. No.:
HY-124637
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