Bardoxolone

Dzina la Chemical:

(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 asidi

SMILES Kodi:

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

InChi kodi:

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

InChi Key:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

Mawu ofunika:

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

Kusungunuka:Zosungunuka mu DMSO

Posungira:0 - 4 ° C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 ° C kwa nthawi yaitali (miyezi).

Kufotokozera:

Zigawo za impso zochokera ku nyani za Bardoxolone methyl-treated zimasonyeza kuchepa kwa mapuloteni a megalin ngakhale kuti mRNA imasonyeza m'magulu onse. Kuchepa kowonekera kwa megalin protein expression kumatsimikiziridwa ndi kusanthula kwa densitometry, komwe kunawonetsa kuti Bardoxolone methyl administration idachepetsa kwambiri megalin protein expression mu impso za nyani. Bardoxolone methyl administration sichimakhudza mapuloteni a cubilin mu impso kapena mRNA mawu a cubilin mu impso. Chilolezo cha creatinine mu nyani zomwe zimayendetsedwa ndi Bardoxolone methyl zimasiyana kwambiri ndi zomwe zimayambira komanso zinyama zomwe zimayendetsedwa ndi galimoto pa tsiku la 28. Pambuyo pa masiku a 28 a Bardoxolone methyl administration, urinary albumin-to-creatinine ratios (UACRs), yotsimikiziridwa kuchokera ku mkodzo wa maola 24. zosonkhanitsira, zikuchulukirachulukira poyerekeza ndi nyama zomwe zimalandira galimoto. Zindikirani, UACRs imachepetsa 53.3% mu zinyama zoyendetsedwa ndi galimoto ndipo inawonjezeka 27.9% mu anyani a Bardoxolone methyl [3]. Amuna a C57BL / 6J mbewa amaperekedwa pakamwa BARD pa nthawi ya HFD kudyetsa (HFD / BARD), amangodyetsa zakudya zamafuta ambiri (HFD), kapena kudyetsedwa zakudya zamafuta ochepa (LFD) kwa masabata a 21. Poyerekeza ndi mbewa za LFD, mbewa za HFD zili ndi chiwonjezeko chodziwika mu kuchuluka kwa F4/80 zomanga ngati korona (+ 95%; p<0.001), yomwe imatetezedwa bwino ndi BARD (-50%; p<0.01). Momwemonso, chiwerengero cha F4/80 interstitial macrophages ndichokwera kwambiri mu mbewa za HFD ndi 98% (p<0.001) poyerekeza ndi mbewa za LFD ndi 32% (p<0.01) poyerekeza ndi mbewa za HFD/BARD[4].

Cholinga: Nrf-2