GSK3335103 | αvβ6 inhibitor | Probechem Biochemicals

Chemical Structure : GSK3335103

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GSK3335103 (GSK-3335103)

货号: PC-72274Not For Human Use, Lab Use Only.

GSK3335103 (GSK-3335103) is a potent, oral, small molecule RGD-mimetic αvβ6 integrin inhibitor with pKi of 9.96.

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生物&药学活性

GSK3335103 (GSK-3335103) is a potent, oral, small molecule RGD-mimetic αvβ6 integrin inhibitor with pKi of 9.96.
GSK3335103 was shown to have a minimum of 4-fold (αvβ3) and a maximum >91,201 (αIIbβ3) selectivity over the other RGD integrins.
GSK3335103 caused a concentration-dependent internalisation of αvβ6 in NHBE cells with a pEC50 of 9.35.
Treatment with GSK3335103 resulted in a concentration-dependent reduction in pSmad2 signalling in NHBE cells with a pIC50 value of 8.19, also inhibited pSmad2 signalling in a concentration-dependent manner with a comparable potency in an ex vivo IPF PCLS system.
GSK3335103 inhibit the activation of TGFβ in a murine model of bleomycin-induced lung fibrosis, as measured by αvβ6 engagement, TGFβ signalling and collagen deposition, with a prolonged duration of action observed in vivo.

物理化学性质&存储条件

分子量	485.6
分子式	C27H36FN3O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-4-((S)-3-fluoro-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)-3-(3-(2-methoxyethoxy)phenyl)butanoic acid

参考文献

1. Alex L Wilkinson, et al. Eur J Pharmacol. 2021 Dec 15;913:174618.

GSK3335103 (GSK-3335103)

生物&药学活性

物理化学性质&存储条件

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GSK3335103 (GSK-3335103)

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物理化学性质&存储条件

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