GSK805|cas:1426802-50-7|西域试剂

GSK805,98.26%

产品编号：Bellancom-12776| CAS NO：1426802-50-7| 分子式：C₂₃H₁₈Cl₂F₃NO₄S| 分子量：532.36

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-12776	￥1600.00	杭州北京（现货）
Bellancom-12776	￥2800.00	杭州北京（现货）
Bellancom-12776	￥5600.00	杭州北京（现货）
Bellancom-12776	￥11000.00	杭州北京（现货）
Bellancom-12776	￥0.00	杭州北京（现货）

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GSK805

产品介绍

GSK805 是一种具有口服活性和中枢神经系统可透性的 RORγt 抑制剂。GSK805 抑制 RORγ 和 Th17 细胞分化，其 pIC₅₀ 为 8.4 和 >8.2。GSK805 抑制 Th17 细胞的功能。GSK805 可用于免疫的研究。

生物活性

GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC₅₀ values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity.

体外研究

GSK805 (0.5 μM; 4 d) inhibits Th17 cell responses.

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

Cell Differentiation Assay

Cell Line:	CD4^{+^{T cells}}
Concentration:	0.5 μM
Incubation Time:	4 days
Result:	Inhibited IL-17 production during Th17 cell differentiation.

体内研究
(In Vivo)

GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE).
GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice.

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

Animal Model:	C57BL/6 mice were immunized with MOG35–55 plus CFA
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once per day; for 35 days
Result:	Efficiently ameliorated the severity of EAE in mice.

Animal Model:	C57BL/6 mice with EAE
Dosage:	30 mg/kg
Administration:	Oral gavage; 30 mg/kg once
Result:	Reduced both IFN-γ^-IL-17⁺ and IFN-γ⁺IL-17⁺ T cells without altered the frequency of TNF-α⁺ T cells in EAE mice.

体内研究

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

Animal Model:	C57BL/6 mice were immunized with MOG35–55 plus CFA
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once per day; for 35 days
Result:	Efficiently ameliorated the severity of EAE in mice.

Animal Model:	C57BL/6 mice with EAE
Dosage:	30 mg/kg
Administration:	Oral gavage; 30 mg/kg once
Result:	Reduced both IFN-γ^-IL-17⁺ and IFN-γ⁺IL-17⁺ T cells without altered the frequency of TNF-α⁺ T cells in EAE mice.

体内研究

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

Animal Model:	C57BL/6 mice were immunized with MOG35–55 plus CFA
Dosage:	10 mg/kg
Administration:	Oral gavage; 10 mg/kg once per day; for 35 days
Result:	Efficiently ameliorated the severity of EAE in mice.

Animal Model:	C57BL/6 mice with EAE
Dosage:	30 mg/kg
Administration:	Oral gavage; 30 mg/kg once
Result:	Reduced both IFN-γ^-IL-17⁺ and IFN-γ⁺IL-17⁺ T cells without altered the frequency of TNF-α⁺ T cells in EAE mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (187.84 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8784 mL	9.3921 mL	18.7843 mL
5 mM	0.3757 mL	1.8784 mL	3.7569 mL
10 mM	0.1878 mL	0.9392 mL	1.8784 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: ≥ 2.5 mg/mL (4.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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% corn oil
Solubility: ≥ 2.5 mg/mL (4.70 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.70 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。