RVX-297|cas:1044871-04-6|西域试剂

RVX-297,96.59%

产品编号：Bellancom-114504| CAS NO：1044871-04-6| 分子式：C₂₄H₂₉N₃O₄| 分子量：423.50

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-114504	￥2500.00	杭州北京（现货）
Bellancom-114504	￥4000.00	杭州北京（现货）
Bellancom-114504	￥8500.00	杭州北京（现货）
Bellancom-114504	￥13500.00	杭州北京（现货）

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RVX-297

产品介绍

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 IC₅₀s 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	Synovial fibroblasts
Concentration:	1-30 μM
Incubation Time:	24 hours
Result:	Downregulated IL-6 and VCAM-1 gene expression in synovial fibroblasts.

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.

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (118.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3613 mL	11.8064 mL	23.6128 mL
5 mM	0.4723 mL	2.3613 mL	4.7225 mL
10 mM	0.2361 mL	1.1806 mL	2.3613 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.91 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.91 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.91 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。