I-Bardoxolone

Igama Lekhemikhali:

(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 i-asidi

Ikhodi ye-SMILES:

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

Ikhodi ye-InChi:

I-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

I-InChi Key:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

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

Incazelo:

Izigaba zezinso ezivela ezinkawini eziphathwa nge-methyl e-Bardoxolone zibonisa ukwehla kwe-megalin protein expression naphezu kwenkulumo efanayo ye-mRNA kuwo wonke amaqembu. Ukuncipha okubonakalayo ekukhulumeni kwamaprotheni e-megalin kuqinisekiswa ukuhlaziywa kwe-densitometry, okubonise ukuthi ukuphathwa kwe-Bardoxolone methyl kunciphisa kakhulu i-megalin protein expression in the monkey kidney. Ukuphathwa kwe-Bardoxolone methyl akuthinti ukubonakaliswa kwamaprotheni e-cubilin ezinso noma inkulumo ye-mRNA ye-cubilin ezinso. Ukukhishwa kwe-creatinine ezinkawini ezilawulwa i-Bardoxolone methyl kuhluke kakhulu kulokho okuyisisekelo kanye nezilwane eziphathwa ngemoto ngosuku lwe-28. Ngemuva kwezinsuku ze-28 zokuphathwa kwe-Bardoxolone methyl, i-urinary albumin-to-creatinine ratios (UACRs), enqunywe kusukela kumchamo wamahora angu-24. amaqoqo, anda kakhulu uma kuqhathaniswa nalawo ezilwane ezithola imoto. Inothi, ama-UACR anciphisa i-53.3% ezilwaneni eziphathwa ngemoto futhi anda ngo-27.9% ezinkawini eziphethwe i-Bardoxolone methyl[3]. Amagundane e-C57BL/6J abesilisa anikezwa i-BARD yomlomo ngesikhathi sokuphakelwa kwe-HFD (HFD/BARD), ondliwe kuphela ukudla okunamafutha aphezulu (HFD), noma ondle ukudla okunamafutha aphansi (LFD) amaviki angu-21. Uma kuqhathaniswa namagundane e-LFD, amagundane e-HFD anokwenyuka okuphawulekayo kwenani lezakhiwo ezinjengomqhele ze-F4/80 (+95%; p<0.001), evinjelwa ngempumelelo yi-BARD (−50%; p<0.01). Ngokufanayo, inani le-F4/80 interstitial macrophage liphezulu kakhulu kumagundane e-HFD ngo-98% (p<0.001) uma kuqhathaniswa namagundane e-LFD futhi ngo-32% (p<0.01) uma kuqhathaniswa namagundane e-HFD/BARD[4].

Ithagethi: Nrf-2