Bardoxolone

Inoa Kimia:

(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 ʻakika

SMILES Code:

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

Code 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

Ki InChi:

TXGZJQLMVSIZEI-UQMAOPSPSA-N

huaʻōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina).

wehewehe:

Hōʻike nā ʻāpana kīʻaha mai Bardoxolone methyl-treated monkey i ka emi ʻana o ka hōʻike protein megalin ʻoiai ke ʻano like o ka mRNA ma waena o nā hui. Ua hōʻoia ʻia ka emi ʻana o ka megalin protein e ka densitometry analyses, ka mea i hōʻike i ka hoʻokele ʻana o Bardoxolone methyl i hoʻemi nui i ka hōʻike protein megalin i loko o ke kīkēkē. ʻAʻole pili ka lawelawe ʻana o Bardoxolone methyl i ka hōʻike protein o cubilin i loko o ka puʻupaʻa a i ʻole ka hōʻike mRNA o cubilin i loko o ka puʻupaʻa. ʻO ka hoʻomaʻemaʻe creatinine i loko o nā monkey i lawelawe ʻia ʻo Bardoxolone methyl he ʻokoʻa loa ia mai kēlā ma ka baseline a me nā holoholona mālama kaʻa i ka lā 28. Ma hope o nā lā 28 o Bardoxolone methyl administration, urinary albumin-to-creatinine ratios (UACRs), i hoʻoholo ʻia mai ka mimi 24-hola. ʻO nā hōʻiliʻili, ua hoʻonui nui ʻia ke hoʻohālikelike ʻia me nā mea i loaʻa i nā kaʻa holoholona. ʻO ka hoʻomaopopo, hoʻemi ka UACR i ka 53.3% i nā holoholona i mālama ʻia i ka kaʻa a hoʻonui i ka 27.9% i nā monkeys Bardoxolone methyl-treated [3]. Hāʻawi ʻia nā ʻiole kāne C57BL/6J i ka BARD waha i ka wā hānai HFD (HFD/BARD), hānai wale ʻia i ka meaʻai momona momona (HFD), a i ʻole i hānai ʻia i ka meaʻai momona haʻahaʻa (LFD) no 21 pule. Ke hoʻohālikelike ʻia me nā ʻiole LFD, loaʻa i nā ʻiole HFD ka piʻi nui ʻana o ka nui o nā hale e like me ka lei aliʻi F4/80 (+95%; p<0.001), i pale pono ia e BARD (−50%; p<0.01). Pēlā nō, ʻoi aku ka kiʻekiʻe o ka nui o F4/80 interstitial macrophages i nā ʻiole HFD e 98% (p<0.001) hoʻohālikelike ʻia me nā ʻiole LFD a me 32% (p<0.01) i hoʻohālikelike ʻia me nā ʻiole HFD/BARD [4].

Kuhikuhi: Nrf-2