Bardoxolone

Magaca Kiimikada:

(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

Koodhka dhoola cadeynta:

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

Koodhka 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

Furaha InChi:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

Ereyga muhiimka ah:

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

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo).

Sharaxaad:

Qaybaha kelyaha ee laga helo Bardoxolone methyl-daayeer lagu daweeyay ayaa muujinaya hoos u dhac ku yimid muujinta borotiinka megalin inkasta oo ay kooxuhu isku mid yihiin. Hoos u dhaca muuqaalka ah ee muujinta borotiinka megalin waxa lagu xaqiijiyay falanqaynta densitometry, taas oo muujisay in maamulka Bardoxolone methyl uu si weyn hoos ugu dhigay muujinta borotiinka megalin ee kelyaha daayeer. Maamulka methyl ee Bardoxolone ma saameynayo muujinta borotiinka ee cubilin ee kelyaha ama muujinta mRNA ee cubilin ee kelyaha. Nadiifinta creatinine ee daanyeerka ee lagu maamulo Bardoxolone methyl si weyn ayey uga duwan tahay tan salka iyo xayawaanka lagu daaweeyay gaadiidka maalinta 28. Ka dib 28 maalmood ee maamulka Bardoxolone methyl, saamiga albumin-to-creatinine kaadida (UACRs), oo lagu go'aamiyay kaadida 24-saac. ururinta, ayaa si weyn u kordhay marka la barbar dhigo kuwa xoolaha helaya gaadiidka. Xusuusnow, UACRs waxay hoos u dhigtaa 53.3% xoolaha lagu daweeyay gaadhi waxayna kordhisay 27.9% daayeerrada Bardoxolone methyl-la daweeyay[3]. Jiirarka labka ah ee C57BL/6J waxa lagu maamulaa BARD afka ah inta lagu jiro quudinta HFD/BARD, kaliya waxa la quudiyay cunto dufan badan (HFD), ama la quudiyo cunto dufanku ku yar yahay (LFD) ilaa 21 toddobaad. Marka la barbardhigo jiirarka LFD, jiirarka HFD waxay leeyihiin koror muuqda oo ah tirada F4/80 qaab-dhismeedka taaj u eg (+95%; p<0.001), kaas oo ay si wax ku ool ah uga hortagto BARD (-50%; p<0.01). Sidoo kale, tirada F4/80 macrophages interstitial ayaa aad uga sarreeya jiirarka HFD 98% (p)<0.001) marka la barbar dhigo jiirarka LFD iyo 32% (p<0.01) marka la barbar dhigo jiirarka HFD/BARD[4].

Bartilmaameedka: Nrf-2