Bardoxolone

Igama leMchiza:

(4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-diox o-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicene-4a-carboxylic iasidi

Ikhowudi yoncumo:

CC(C)([C@](CC[C@@]([C@@]1(CC[C@]2(CCC(C)(C[C@]2([C@]13[H ])[H])C)C(O)=O)C)4C)5[H])C(C(C#N)=C[C@]5(C)C4=CC3=O)=O

Ikhowudi ye-InChi:

InChI=1S/C31H41NO4/c1-26(2)10-12-31(25(35)36)13-11-30(7)23(19(31)16-26)20(33)14-22- 28(5)15-18(17-32)24(34 )27(3,4)21(28)8-9-29(22,30)6/h14-15,19,21,23H,8-13,16H2,1-7H3,(H,35,36) /t19-,21-,23-,28-,29+,30+,31-/m0/s1

Isitshixo se-InChi:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

Igama elingundoqo:

Bardoxolone, RTA 402, CCDO, RTA-402, RTA402, 218600-44-3

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).

Inkcazo:

Amacandelo ezintso ezivela kwi-Bardoxolone methyl-treated monkeys ibonisa ukunciphisa i-megalin protein expression nangona i-mRNA ibonakaliso efanayo kumaqela. Ukuncipha okubonakalayo kwinkcazo yeprotheyini ye-megalin iqinisekiswa ngokuhlalutya kwe-densitometry, ebonisa ukuba ulawulo lwe-Bardoxolone methyl lunciphisa kakhulu i-megalin protein expression kwi-monkey kidney. Ulawulo lwe-Bardoxolone methyl aluchaphazeli ukubonakaliswa kweprotheyini ye-cubilin kwizintso okanye ukubonakaliswa kwe-mRNA ye-cubilin kwizintso. Ukukhutshwa kwe-creatinine kwiinkawu ezilawulwa yi-Bardoxolone methyl yahluke kakhulu kwisiseko kunye nezilwanyana eziphathwa ngemoto ngosuku lwe-28. Emva kweentsuku ze-28 zolawulo lwe-Bardoxolone methyl, i-urinary albumin-to-creatinine ratios (UACRs), enqunywe ukusuka kumchamo weeyure ze-24. ingqokelela, yande kakhulu xa ithelekiswa nezo zezilwanyana ezifumana isithuthi. Inqaku, i-UACRs iyancipha i-53.3% kwizilwanyana eziphathwa ngemoto kwaye yanda i-27.9% kwi-monkeys ye-Bardoxolone methyl [3]. Iigundane ze-C57BL / 6J zamadoda zilawulwa ngomlomo we-BARD ngexesha lokutya kwe-HFD (HFD / BARD), kuphela ukutya okunamafutha aphezulu (HFD), okanye ukutya okunamafutha aphantsi (LFD) kwiiveki ze-21. Xa kuthelekiswa neempuku ze-LFD, iimpuku ze-HFD zinokunyuka okuphawulweyo kwinani le-F4/80 yezakhiwo ezifana nesithsaba (+95%; p<0.001), ethintelwa ngokufanelekileyo yi-BARD (-50%; p<0.01). Ngokufanayo, inani le-F4/80 interstitial macrophages liphezulu kakhulu kwiimpuku ze-HFD nge-98% (p<0.001) xa kuthelekiswa neempuku ze-LFD kunye ne-32% (iphe<0.01) xa kuthelekiswa neempuku ze-HFD/BARD[4].

Ithagethi: Nrf-2