Bardoxolone

Lebitso la lik'hemik'hale:

(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 asiti

SMILES Khouto:

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

Khoutu ea 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

InChi Key:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

Keyword:

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

Sollubility:E qhibiliha ka DMSO

Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli).

Tlhaloso:

Likarolo tsa liphio tse tsoang litšoeneng tsa Bardoxolone methyl-treated li bontša ho fokotseha ha protheine ea megalin ho sa tsotellehe polelo e tšoanang ea mRNA ho pholletsa le lihlopha. Ho fokotseha ho bonahalang ha protheine ea megalin ho tiisoa ke litlhahlobo tsa densitometry, tse bontšitseng hore tsamaiso ea Bardoxolone methyl e fokolitse haholo polelo ea protheine ea megalin liphio tsa monkey. Tsamaiso ea methyl ea Bardoxolone ha e ame polelo ea protheine ea cubilin liphio kapa polelo ea mRNA ea cubilin liphio. Ho tlosoa ha creatinine ho litšoene tse tsamaisoang ke Bardoxolone methyl ho ne ho fapane haholo le ho tloha qalong le liphoofolong tse tšoaroang ka koloi letsatsing la 28. Ka mor'a matsatsi a 28 a tsamaiso ea Bardoxolone methyl, urinary albumin-to-creatinine ratios (UACRs), e khethiloeng ho tloha morong oa lihora tsa 24. likoleke, li eketseha haholo ha li bapisoa le tsa likoloi tse amohelang liphoofolo. Ela hloko, UACRs e fokotsa 53.3% ho liphoofolo tse tšoaroang ke koloi 'me e eketsehile 27.9% ho litšoene tse tšoaroang ke methyl ea Bardoxolone [3]. Litoeba tse tona tsa C57BL / 6J li tsamaisoa ka molomo BARD nakong ea ho fepa HFD (HFD / BARD), feela ho fepa lijo tse nang le mafura a mangata (HFD), kapa ho fepa lijo tse tlaase (LFD) bakeng sa libeke tsa 21. Ha ho bapisoa le litoeba tsa LFD, litoeba tsa HFD li na le keketseho e hlakileng ea palo ea meaho e kang moqhaka oa F4/80 (+95%; p<0.001), e thibetsoeng ka katleho ke BARD (-50%; leq<0.01). Ka mokhoa o ts'oanang, palo ea F4/80 interstitial macrophages e phahame haholo ho litoeba tsa HFD ka 98% (leq.<0.001) ha e bapisoa le litoeba tsa LFD le 32% (leq<0.01) ha e bapisoa le litoeba tsa HFD/BARD[4].

Sepheo: Nrf-2