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FR900359
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FR900359图片
CAS NO:107530-18-7
包装:1mg
市场价:4914元

产品介绍
A cyclic depsipeptide and an inhibitor of Gαq, Gα11, and Gα14<•sub>
Cas No.107530-18-7
Canonical SMILESCCC(N[C@@H]([C@H](O)C(C)C)C(O[C@@H]([C@@]1([H])C(N([C@@](C(O[C@@H]([C@@H](C(O[C@@H](C(N(C(C(N[C@H](C(N([C@H](C(N1)=O)C)C)=O)C)=O)=C)C)=O)CC2=CC=CC=C2)=O)NC(C)=O)C(C)C)=O)([H])[C@@H](C)OC)C)=O)C(C)C)=O)=O
分子式C49H75N7O15
分子量1002.2
溶解度Chloroform: soluble
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

FR900359 is a cyclic depsipeptide that has been found inA. crenataand is an inhibitor of Gαq, Gα11, and Gα14(IC50s = 13.18, 10.47, and 10 nM, respectively).1,2It is selective for these Gα subunits over a panel of additional Gα subunits, including Gαsand Gαi, in bioluminescence resonance energy transfer (BRET) assays at 1 µM.3FR900359 (1 µM) induces relaxation of precontracted isolated mouse tail arteries and inhibits platelet aggregation induced by U-46619 in washed isolated human platelets cultured with aspirin in a concentration-dependent manner.3,4It induces cell cycle arrest at the G1phase and reduces proliferation and serum-induced migration of B16 melanoma cells.3FR900359 (2.5 µg/animal) inhibits airway hyperresponsiveness in a mouse model of house dust mite-induced allergic asthma.5

1.Fujioka, M., Koda, S., Morimoto, Y., et al.Structure of FR900359, a cyclic depsipeptide from Ardisia crenata simsJ. Org. Chem.53(12)2820-2825(1988) 2.Kukkonen, J.P.G-protein inhibition profile of the reported Gq/11 inhibitor UBO-QICBiochem. Biophys. Res. Commun.469(1)101-107(2016) 3.Schrage, R., Schmitz, A.-L., Gaffal, E., et al.The experimental power of FR900359 to study Gq-regulated biological processesNat. Commun.610156(2015) 4.Inamdar, V., Patel, A., Manne, B.J., et al.Characterization of UBO-QIC as a Gαq inhibitor in plateletsPlatelets26(8)771-778(2015) 5.Matthey, M., Roberts, R., Seidinger, A., et al.Targeted inhibition of Gq signaling induces airway relaxation in mouse models of asthmaSci. Transl. Med.9(407)eaag2288(2017)