RVX-297

≥96%

CAS编号: 1044871-04-6
分子式: C₂₄H₂₉N₃O₄
分子量: 423.50
PubChem编号: 135567084

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货号 (SKU)	包装规格	是否现货
R647899-5mg	5mg	期货
R647899-10mg	10mg	期货
R647899-25mg	25mg	期货
R647899-50mg	50mg	期货

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Epigenetic Reader Domain (260) 表观遗传学 (1496)

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基本描述

规格或纯度	≥96%
英文名称	RVX-297
生化机理	RVX-297 是一种强效的口服活性 BET 溴结构域抑制剂，对 BD2 具有选择性。RVX-297 对 BRD2（BD2）、BRD3（BD2）和 BRD4（BD2）的 IC 50 s 分别为 0.08、0.05 和 0.02 μM。RVX-297 可抑制多种免疫缺陷病毒的炎症基因表达
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	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. Form:Solid

关联靶点（人）

BRD4 Tchem 含溴结构域蛋白 4(Bromodomain-containing protein 4) (1 活性数据)

点击查看靶蛋白信息： BRD4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 (13122 活性数据)

点击查看靶蛋白信息： BRD4

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

IL1B Tclin Interleukin-1 beta (9 活性数据)

点击查看靶蛋白信息： IL1B

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	未知
IUPAC Name	2-[3,5-dimethyl-4-(2-pyrrolidin-1-ylethoxy)phenyl]-5,7-dimethoxy-3H-quinazolin-4-one
INCHI	InChI=1S/C24H29N3O4/c1-15-11-17(12-16(2)22(15)31-10-9-27-7-5-6-8-27)23-25-19-13-18(29-3)14-20(30-4)21(19)24(28)26-23/h11-14H,5-10H2,1-4H3,(H,25,26,28)
InChi Key	PQZDYFRDRHRZGF-UHFFFAOYSA-N
Canonical SMILES	CC1=CC(=CC(=C1OCCN2CCCC2)C)C3=NC4=C(C(=CC(=C4)OC)OC)C(=O)N3
Isomeric SMILES	CC1=CC(=CC(=C1OCCN2CCCC2)C)C3=NC4=C(C(=CC(=C4)OC)OC)C(=O)N3
PubChem CID	135567084
MeSH Entry Terms	RVX-297
分子量	423.50

化学和物理性质

溶解性	DMSO : 50 mg/mL (118.06 mM; Need ultrasonic)
分子量	423.500 g/mol
XLogP3	3.500
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	6
可旋转键计数Rotatable Bond Count	7
精确质量Exact Mass	423.216 Da
单同位素质量Monoisotopic Mass	423.216 Da
拓扑极表面积Topological Polar Surface Area	72.400 Å²
重原子数Heavy Atom Count	31
形式电荷Formal Charge	0
复杂度Complexity	639.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

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基本描述

关联靶点（人）

作用机制

名称和识别符

化学和物理性质

安全和危险性（GHS）

质量标准

质检证书（CoA,COO,BSE/TSE 和分析图谱)

溶液计算器

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