I-GLPG0187

Igama Lekhemikhali:

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

Ikhodi ye-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

Ikhodi ye-InChi:

I-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

I-InChi Key:

CXHCNOMGODVIKB-VWLOTQADSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

Ekuhlolweni kwesigaba esiqinile, i-GLPG0187 ibonisa ukukhetha kwama-RGD integrin receptors amaningana ane-IC50s ye-1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM ye-αvβ1, αvβ3, αvβ5, αvβ6, αvβ8, kanye ne-αvβ8, kanye ne-αvβ8, ne-αvβ8. I-GLPG0187 iyisivimbeli esinamandla se-osteoclastic bone resorption kanye ne-angiogenesis. Ukwelashwa nge-GLPG0187 kuncike kumthamo kukhulisa isilinganiso se-E-cadherin/vimentin, kunikeza amaseli i-epithelial, i-sessile phenotype. I-GLPG0187 incike kumthamo wehlisa usayizi we-aldehyde dehydrogenase ephezulu yokugcwala kwamaseli omdlavuza wendlala yesinye [1]. Ukwelashwa kwe-GLPG0187 kuphumela ekuhlanganisweni kwamaseli kanye nokunqwabelana. I-GLPG0187 ibonisa ukwehla okubalulekile okuncike kumthamo ekufudukeni kweseli yesimila. I-GLPG0187 kukho konke ukugxila kunciphisa kakhulu ukwanda kwamaseli[2].

Ithagethi: αvβ1