RN486|cas:1242156-23-5|西域试剂

RN486,99.87%

产品编号：Bellancom-18018| CAS NO：1242156-23-5| 分子式：C₃₅H₃₅FN₆O₃| 分子量：606.69

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-18018	￥900.00	杭州北京（现货）
Bellancom-18018	￥1600.00	杭州北京（现货）
Bellancom-18018	￥3000.00	杭州北京（现货）
Bellancom-18018	￥6000.00	杭州北京（现货）
Bellancom-18018	￥9600.00	杭州北京（现货）

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产品介绍

RN486 是一种有效的，选择性的，具有口服活性的 Btk 抑制剂，IC₅₀ 为 4.0 nM，K_d 为 0.31 nM，对其他激酶的活性较低。RN486 可用于类风湿关节炎和系统性红斑狼疮的研究。

生物活性

RN486 is a potent, selective and orally active Btk inhibitor with an IC₅₀ of 4.0 nM and a K_d of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.

体外研究

RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC₅₀ = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC₅₀ = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC₅₀ = 21 nM).
In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486.

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

体内研究

RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 24 mg/mL (39.56 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6483 mL	8.2414 mL	16.4829 mL
5 mM	0.3297 mL	1.6483 mL	3.2966 mL
10 mM	0.1648 mL	0.8241 mL	1.6483 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。

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
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

. Xu D, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. [Content Brief]

. Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104. [Content Brief]

. Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91. [Content Brief]

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RN486,99.87%

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