WAY-204688 SIM-688|cas:796854-35-8|西域试剂

WAY-204688 SIM-688,99.06%

产品编号：Bellancom-19498| CAS NO：796854-35-8| 分子式：C₃₄H₃₁F₃N₂O₂| 分子量：556.62

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货号	价格	库存与货期
Bellancom-19498	￥4900.00	杭州北京（现货）
Bellancom-19498	￥9900.00	杭州北京（现货）
Bellancom-19498	￥15800.00	杭州北京（现货）

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WAY-204688 SIM-688

产品介绍

WAY-204688 是雌激素受体 (ER-α) 选择性的，口服活性的 NF-κB 转录活性抑制剂。在 HAECT 细胞中，作用于NF-κB-Luc 荧光素酶，IC₅₀ 为 122 ± 30 nM。

生物活性

WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC₅₀ of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.

体外研究

WAY-204688 is ER-dependenrt (activity seen only when hER is coexpressed with NF-κB-luciferase in human aortic endothelial cell lines (HAECT-1) cells). The interaction of WAY-204688 with ERα and ERβ is examined in vitro. WAY-204688 displaces [³H]E2 from the ERα ligand binding domain protein (LBD) with IC₅₀=2.43 μM and from the ERβ ligand binding domain protein (LBD) with IC₅₀=1.5 μM.

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

体内研究

WAY-204688 (5 mg/kg per day, po daily for 5 weeks) is evaluated in vivo for the ability to inhibit four proinflammatory genes (MHC, invariant chain (MHI), VCAM-1, RANTES, and TNF-α). The effect of WAY-204688 on induction of the gene products and on uterine wet weight is compared to that of 17α-ethinyl 17β-estradiol (EE at 10 μg/kg per day) in the same paradigm. Further characterization of WAY-204688 is carried out in several preclinical models of inflammatory disease. In the Lewis rat adjuvant-induced arthritis model (AIA), WAY-204688 is active at a dose of 0.3 mg/kg per day, po.

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 : 100 mg/mL (179.66 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7966 mL	8.9828 mL	17.9656 mL
5 mM	0.3593 mL	1.7966 mL	3.5931 mL
10 mM	0.1797 mL	0.8983 mL	1.7966 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 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.49 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。