RVX-297|1044871-04-6|-陌孚医药/Medlife

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RVX-297

目录号: PL02231 纯度: ≥96%

CAS No. :1044871-04-6

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中文名称	RVX-297
英文名称	RVX-297
英文别名	2-{3,5-Dimethyl-4-[2-(Pyrrolidin-1-Yl)ethoxy]phenyl}-5,7-Dimethoxyquinazolin-4(3h)-One;2-(3,5-dimethyl-4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)-5,7-dimethoxyquinazolin-4(3h)-one;5GD;RVX297;BDBM50511879;Q27455739;2-[3,5-dimethyl-4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,7-dimethoxy-1H-quinazolin-4-one;2-[3,5-dimethyl-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-5,7-dimethoxy-4(3H)-Quinazolinone;RVX-297
Cas No.	1044871-04-6
分子式	C₂₄H₂₉N₃O₄
分子量	423.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	RVX-297 是一种高效、具有口服活性、对 BD2 有选择性的 BET 抑制剂。RVX-297 对 BRD2(BD2)，BRD3(BD2)，BRD4(BD2) 的 IC₅₀ 分别为 0.08、0.05、0.02 μM。RVX-297 抑制多种免疫细胞炎症基因的表达。RVX-297 对临床前模型急性炎症和自身免疫的有效。
生物活性	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.
性状	Solid
IC50 & Target[1][2]	BRD2 (BD1) 3.76 μM (IC50) BRD2 (BD2) 0.08
体外研究(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 IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression.M
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Jahagirdar R, et al. RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease. Mol Pharmacol. 2017;92(6):694-706. [2]. Kharenko OA, et al. RVX-297- a novel BD2 selective inhibitor of BET bromodomains. Biochem Biophys Res Commun. 2016;477(1):62-67.

溶解度数据	In Vitro: DMSO : 50 mg/mL (118.06 mM; Need ultrasonic)配制储备液

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