FR900359

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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。

CAS NO:	107530-18-7
包装:	1mg
市场价:	4914元

A cyclic depsipeptide and an inhibitor of Gα_q, Gα₁₁, and Gα_{14<•sub>Cas No. 107530-18-7
Canonical SMILES CCC(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 tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation 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 Gα_q, 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 Gα_sand Gα_i, 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)}

Cas No.	107530-18-7
Canonical SMILES	CCC(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 tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation 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 Gα_q, 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 Gα_sand Gα_i, 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)