| Identification | Back Directory | [Name]
L-Threonine,(3R)-N-acetyl-3-hydroxy-L-leucyl-(aR)-a-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-L-leucyl-N,O-dimethyl-,(7(R)1)-lactone (9CI) | [CAS]
107530-18-7 | [Synonyms]
L-Threonine,(3R)-N-acetyl-3-hydroxy-L-leucyl-(aR)-a-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pent
L-Threonine, (3R)-N-acetyl-3-hydroxy-L-leucyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone
L-Threonine,(3R)-N-acetyl-3-hydroxy-L-leucyl-(aR)-a-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-3-hydroxy-4-methyl-1-oxo-2-[(1-oxopropyl)amino]pentyl]oxy]-L-leucyl-N,O-dimethyl-,(7(R)1)-lactone (9CI) | [Molecular Formula]
C49H75N7O15 | [MOL File]
107530-18-7.mol | [Molecular Weight]
1002.16 |
| Hazard Information | Back Directory | [Uses]
FR900359 is a depsipeptide selective inhibitor of Gαq/11/14 in mammalia, can inhibits ERK pathway. FR900359 suppresses the proliferation of melanoma cells and decreases of blood pressure. FR900359 also protected against airway hyperreactivity in murine models of allergen sensitization in Ovalbumins(HY-W250978)–induced sensitization model of asthma. FR900359 can be used for cancer and cardiovascular disease research[1][2][3][4]. | [Definition]
ChEBI: FR900359 is a cyclodepsipeptide. | [in vivo]
FR900359 (0.2 or 1 mg/ml, 12 μL per mouse, i.v.) strongly reduces vascular tone in mouse tail artery[1].
FR900359 (0.1 mg/ml, 2.5 mg/mouse, intratracheally) abolishes airway hyperreactivity after Ovalbumin (HY-W250978)-induced sensitization in mice[4].
| Animal Model: | Isometric force measurements in mouse tail artery [1] | | Dosage: | 1.0 μM | | Administration: | Washed | | Result: | Strongly reduced vascular tone
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| Animal Model: | Ovalbumins–induced sensitization model of asthma. [4] | | Dosage: | 0.1 mg/ml, 2.5 mg per mouse | | Administration: | Intratracheally | | Result: | Abolished airway hyperreactivity after ovalbumin-induced sensitization in mice
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| [storage]
-20°C | [References]
[1] Schrage R, et.al. The experimental power of FR900359 to study Gq-regulated biological processes. Nat Commun. 2015 Dec 14;6:10156. DOI:10.1038/ncomms10156
[2] Fujioka, M,et.al. Structure of FR900359, a cyclic depsipeptide from Ardisia crenata sims J. Org. Chem. 1988, 53 (12), 2820?2825.
[3] Lapadula D, et.al. Effects of Oncogenic Gαq and Gα11 Inhibition by FR900359 in Uveal Melanoma. Mol Cancer Res. 2019 Apr;17(4):963-973. DOI:10.1158/1541-7786.MCR-18-0574
[4] Matthey M, et.al. Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthma. Sci Transl Med. 2017 Sep 13;9(407):eaag2288. DOI:10.1126/scitranslmed.aag2288 |
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