1. Neuronal Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  2. Trk Receptor Akt ERK
  3. Gambogic amide

Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke.

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Gambogic amide Chemical Structure

Gambogic amide Chemical Structure

CAS No. : 286935-60-2

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Description

Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke[1].

In Vitro

Gambogic amide (0.5 μM; 30 min) elicits TrkA tyrosine phosphorylation in hippocampal neurons[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Hippocampal neurons
Concentration: 500 nM
Incubation Time: 30 min
Result: Triggered TrkA Y490 phosphorylation.
In Vivo

Gambogic amide (2 mg/kg; sc; single dose) prevents neuronal cell death and decreases infarct volume in MCAO animal model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCAO mice model[1]
Dosage: 2 mg/kg
Administration: s.c.; 5 min before the onset of reperfusion, after 2 h of MCAO followed by reperfusion; followed by 25 mg/kg Kainic acid (KA)
Result: Diminished Kainic acid-triggered hippocampal neuronal cell death.
Reduces infarct volume in MCAO rat brain.
Molecular Weight

627.77

Formula

C38H45NO7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

NC(/C(C)=C\C[C@@]12[C@]34C(C(C5=C(O)C(C=C[C@](CC/C=C(C)/C)(C)O6)=C6C(C/C=C(C)\C)=C5O3)=O)=C[C@H](C[C@H]4C(C)(C)O2)C1=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 68 mg/mL (108.32 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 1.5929 mL 7.9647 mL 15.9294 mL
5 mM 0.3186 mL 1.5929 mL 3.1859 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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Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

References

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 1.5929 mL 7.9647 mL 15.9294 mL 39.8235 mL
5 mM 0.3186 mL 1.5929 mL 3.1859 mL 7.9647 mL
10 mM 0.1593 mL 0.7965 mL 1.5929 mL 3.9824 mL
15 mM 0.1062 mL 0.5310 mL 1.0620 mL 2.6549 mL
20 mM 0.0796 mL 0.3982 mL 0.7965 mL 1.9912 mL
25 mM 0.0637 mL 0.3186 mL 0.6372 mL 1.5929 mL
30 mM 0.0531 mL 0.2655 mL 0.5310 mL 1.3275 mL
40 mM 0.0398 mL 0.1991 mL 0.3982 mL 0.9956 mL
50 mM 0.0319 mL 0.1593 mL 0.3186 mL 0.7965 mL
60 mM 0.0265 mL 0.1327 mL 0.2655 mL 0.6637 mL
80 mM 0.0199 mL 0.0996 mL 0.1991 mL 0.4978 mL
100 mM 0.0159 mL 0.0796 mL 0.1593 mL 0.3982 mL
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Help & FAQs
  • 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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Product Name:
Gambogic amide
Cat. No.:
HY-121833
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