| Identification | Back Directory | [Name]
GaMbogic aMide | [CAS]
286935-60-2 | [Synonyms]
CID 25252739
GaMbogic aMide
2-Butenamide, 2-methyl-4-[(1R,3aS,5S,11R,14aS)-3a,4,5,7-tetrahydro-8-hydroxy-3,3,11-trimethyl-13-(3-methyl-2-buten-1-yl)-11-(4-methyl-3-penten-1-yl)-7,15-dioxo-1,5-methano-1H,3H,11H-furo[3,4-g]pyrano[3,2-b]xanthen-1-yl]-, (2Z)- | [Molecular Formula]
C38H45NO7 | [MOL File]
286935-60-2.mol | [Molecular Weight]
627.77 |
| Chemical Properties | Back Directory | [Boiling point ]
823.893±65.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.278±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Yellow-orange solid. | [pka]
6.785±0.70(predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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 vivo]
Gambogic amide (2 mg/kg; sc; single dose) prevents neuronal cell death and decreases infarct volume in MCAO animal model[1]. | 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. |
| [References]
[1] Jang SW, et al. Gambogic amide, a selective agonist for TrkA receptor that possesses robust neurotrophic activity, prevents neuronal cell death. Proc Natl Acad Sci U S A. 2007 Oct 9;104(41):16329-34. DOI:10.1073/pnas.0706662104 |
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