RVX-297CAS号： 1044871-04-6分子式： C24H29N3O4分子量： 423.5描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
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.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO:40 mg/ml(94.45 mM)
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| 生物活性 | |
| 靶点 |
BRDT (BD1):2.69 μM, BRD3 (BD1):2.34 μM, BRD4 (BD2):0.02 μM, BRD2 (BD1):3.76 μM, BRD3 (BD2):0.05 μM, BRD4 (BD1):1.16 μM, BRD2 (BD2):0.08 μM
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| In vitro(体外研究) |
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].
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| In vivo(体内研究) |
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].
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