RVX-297 是口服具有活性的，对BD2有选择性的BET高效抑制剂，作用于BRD2(BD2)、BRD3(BD2)、BRD4(BD2) 的IC50分别为 0.08、0.05、0.02 μM。它能够阻碍多种免疫细胞炎症基因的表达，对临床前模型急性炎症及自身免疫均有效。

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

RVX-297 suppressed IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner[2].

In the rCIA model, RVX-297 treatment had a substantial impact on cytokine gene expression; expressions of IL-1β, RANKL, MMP3, and MMP13 were all significantly decreased in the ankle joints of arthritic rats after RVX-297 treatment at 75 mg/kg BID versus vehicle-treated arthritic controls[2].

1044871-04-6

C24H29N3O4

423.5

RVX297;RVX-297

DMSO:40 mg/ml(94.45 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years