GLPG0187

Non Chimik:

(S)-3-((2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pirimidin-4-) yl) amino) -2-((4-methoxyphenyl)sulfonamido)propanoic asid

Kòd SMILES:

O=C(O)[C@H](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC= C(OC)C=C5)=O

Kòd InChi:

InChI=1S/C29H37N7O5S/c1-18-26(31-17-25(29(37)38)35-42(39,40)23-9-7-22(41-3)8-10-23) 32-19(2)33-28(18)36-15-12-20(13-16-36)24-11-6-21-5-4-14-30-27(21)34-24/ h6-11,20,25,35H,4-5,12-17H2,1-3H3,(H,30,34)(H,37,38)(H,31,32,33)/t25-/m0 /s1

InChi kle:

CXHCNOMGODVIKB-VWLOTQADSA-N

Mot:

GLPG0187, GLPG-0187, GLPG 0187, 1320346-97-1

Solibilite:Soluble nan DMSO

Depo:0 - 4 ° C pou kout tèm (jou a semèn), oswa -20 ° C pou tèm long (mwa).

Deskripsyon:

Nan yon tès solid-faz, GLPG0187 montre selektivite pou plizyè reseptè entegrin RGD ak IC50s nan 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM pou αvβ1, αvβ3, αvβ5, αvβ6, αvβ1, ak αvβ8. GLPG0187 se yon inibitè ki pisan nan resorption zo osteoclastic ak anjyogenesis. Tretman ak GLPG0187 dòz-depandan ogmante rapò E-cadherin/vimentin, rann selil yo yon fenotip plis epitelyal, sesil. GLPG0187 depann de dòz la diminye gwosè aldehyde dehydrogenase segondè subpopulation selil kansè pwostat [1]. Tretman GLPG0187 rezilta nan awondi selilè ak asanblaj. GLPG0187 demontre yon rediksyon enpòtan ki depann de dòz la nan migrasyon selil timè yo. GLPG0187 nan tout konsantrasyon siyifikativman diminye pwopagasyon selil [2].

Sib: αvβ1