Bardoxolone methyl

Ingoa matū:

(4aS,6aR,6bS,8aR,12aS,14aR,14bS)-methyl 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-carboxylate

Waehere SMILES:

O=C([C@]1(CC[C@@]2(C)[C@]3(C)CCC4C(C)(C)C(C(C#N)=C[C@]4 (C)C3=C5)=O)CCC(C)(C)C[C@]1([H])[C@@]2([H])C5=O)OC

Waehere InChi:

InChI=1S/C32H43NO4/c1-27(2)11-13-32(26(36)37-8)14-12-31(7)24(20(32)17-27)21(34)15- 23-29(5)16-19(18-33)25(35)28(3,4)22(29)9-10-30(23,31)6/h15-16,20,22,24H, 9-14,17H2,1-8H3/t20-,22?,24+,29+,30-,31-,32+/m1/s1

Kī InChi:

WPTTVJLTNAWYAO-OROHISIGSA-N

Kupumatua:

Bardoxolone methyl, RTA-402, RTA 402, RTA402, NSC-713200, TP-155C, Methyl-CDDO, MethylCDDO, Methyl CDDO, CDDO methyl ester, 218600-53-4

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama)

Whakaahuatanga:

Ko te synthetic oleanane triterpenoid CDDO (Tuemi Nama 81035) he kaiwhakaoho Nrf2 e aukati ana i te tipu me te whakaawe i te rereketanga me te apoptosis i roto i nga momo pukupuku pukupuku. Ko te C-28 methyl ester o te CDDO (CDDO methyl ester) ka aukati i te whakahiato pūtau o te inducible nitric oxide synthase (iNOS) me te COX-2 inducible i roto i nga macrophages kiore INF-γ-whakahohe me te uara IC50 o 0.11 nM. Ka whakaawehia te apoptosis, ka whakaheke i te rereketanga, ka aukati i te urupare mumura i roto i nga momo pukupuku pukupuku na roto i te whakakore i te tohu IκBα kinase / NF-κB. Ko te CDDO methyl ester he mahi antidiabetic kaha, he whakaheke i te whakaaturanga cytokine proinflammatory i roto i nga kiore mate huka momo 2 ngako kai-whangai nui me nga kiore Leprdb / db me te whakaoho i te kinase protein-whakahohe AMP me te LKB1 whakahohe i roto i te uaua me te ate.

Whāinga: NF-kB