Bardoxolone

Chemical Name:

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

SMILES Kodhi:

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 Code:

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

Solubility:Soluble muDMSO

Kuchengeta:0 - 4 ° C kwenguva pfupi (mazuva kusvika mavhiki), kana -20 ° C kwenguva refu (mwedzi).

Tsanangudzo:

Zvikamu zvetsvo kubva kuBardoxolone methyl-treated monkeys inoratidza yakaderera megalin protein kutaura pasinei nemRNA yakafanana kutaura mumapoka. Kuderera kunoonekwa mu megalin protein kutaura kunosimbiswa ne densitometry analyses, iyo yakaratidza kuti Bardoxolone methyl administration yakaderera zvakanyanya megalin protein kutaura mumonkey itsvo. Bardoxolone methyl administration haikanganisi mapuroteni ekutaura kwe cubilin muitsvo kana mRNA kutaura kwecubilin mutsvo. The creatinine clearance mumonke inotungamirirwa neBardoxolone methyl yakasiyana zvakanyanya kubva kune iyo yekutanga uye mumhuka dzinobatwa nemotokari pazuva 28. Mushure memazuva 28 eBardoxolone methyl administration, urinary albumin-to-creatinine ratios (UACRs), yakatemwa kubva kumvura ye24-awa. miunganidzwa, inowedzerwa zvakanyanya kana ichienzaniswa neiyo iri mumhuka dzinogamuchira mota. Cherechedza, UACRs inoderedza 53.3% mumhuka dzinobatwa nemotokari uye yakawedzera 27.9% muBardoxolone methyl-treated monkeys [3]. Murume C57BL / 6J mice inopiwa nemuromo BARD panguva yeHFD kudya (HFD / BARD), inongodyiswa kudya kwemafuta akawanda (HFD), kana kudyiswa pasi-fat diet (LFD) kwevhiki dze21. Kuenzaniswa neLFD mbeva, HFD mbeva dzine kuwedzera kwakakura kwenhamba yeF4/80 korona-yakafanana zvimiro (+ 95%; p.<0.001), iyo inodzivirirwa zvinobudirira neBARD (-50%; p<0.01). Saizvozvo, nhamba yeF4/80 interstitial macrophages yakanyanya kukwirira muHFD mbeva ne98% (p.<0.001) ichienzaniswa neLFD mice uye ne32% (p<0.01) zvichienzaniswa neHFD/BARD mbeva[4].

Chinangwa: Nrf-2