GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.10mM in DMSO
Moligand™,10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Panoramica
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC 50 s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
In Vitro
RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts. RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs. RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses 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. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC 50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC 50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: Synovial fibroblasts Concentration: 1-30 μM Incubation Time: 24 hours Result: Downregulated IL-6 and VCAM-1 gene expression in synovial fibroblasts.
In Vivo
RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model . RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model . RVX-297 suppresses cytokine production in LPS-treated mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis) Dosage: 25, 50, and 75 mg/kg Administration: P.o.; per day for 6 days Result: Prevented swelling and inflammation of the ankle and knee joints.
Specifications
Specifiche e purezza
Moligand™,10mM in DMSO
Meccanismi biochimici e fisiologici
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2 . RVX-297 shows IC 50 s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple imm
Condizioni di conservazione di stoccaggio
Store at -80°C
Spedito in
Dry ice packs + Cold packs
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