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Gambogic amide

Names

[ CAS No. ]:
286935-60-2

[ Name ]:
Gambogic amide

[Synonym ]:
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)-
gambogic amide
(2Z)-4-[(1S,2S,8R,17S,19R)-12-Hydroxy-8,21,21-trimethyl-5-(3-methyl-2-buten-1-yl)-8-(4-methyl-3-penten-1-yl)-14,18-dioxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,&#xD; 11,15-pentaen-19-yl]-2-methyl-2-butenamide

Biological Activity

[Description]:

A potent, selective high affinity TrkA receptor agonist with Kd of 75 nM; selectively binds to TrkA, but not TrkB or TrkC, and robustly induces its tyrosine phosphorylation and downstream signaling activation, including Akt and MAPKs; potently represses cyclin A1 expression and blocks K562 cell proliferation; diminishes kainic acid-triggered neuronal cell death and decreases infarct volume in the transient middle cerebral artery occlusion model of stroke in mice.

[References]

References 1. Jang SW, et al. Proc Natl Acad Sci U S A. 2007 Oct 9;104(41):16329-34. 2. Chan CB, et al. Oncogene. 2009 Oct 29;28(43):3825-36. 3. Obianyo O, et al. Biochim Biophys Acta. 2013 Oct;1834(10):2213-8. View Related Products by Target Trk Receptor

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
823.9±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C38H45NO7

[ Molecular Weight ]:
627.766

[ Flash Point ]:
452.1±34.3 °C

[ Exact Mass ]:
627.319580

[ LogP ]:
9.24

[ Vapour Pressure ]:
0.0±3.1 mmHg at 25°C

[ Index of Refraction ]:
1.627


Related Compounds

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