T6167923|cas:2437475-16-4|西域试剂

T6167923,99.08%

产品编号：Bellancom-19744| CAS NO：2437475-16-4| 分子式：C₁₇H₂₀BrN₃O₃S₂| 分子量：458.39

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-19744	￥1900.00	杭州北京（现货）
Bellancom-19744	￥5600.00	杭州北京（现货）
Bellancom-19744	￥9500.00	杭州北京（现货）
Bellancom-19744	￥15000.00	杭州北京（现货）
Bellancom-19744	￥25000.00	杭州北京（现货）

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T6167923

产品介绍

T6167923 是一种选择性的 MyD88 依赖型信号通路的抑制剂。T6167923 直接与 MyD88 的 Toll/IL1 受体 (TIR) 结构域结合，破坏 MyD88 的同二聚体形成。T6167923 抑制 NF-κB 驱动的葡萄球菌肠毒素AP (SEAP) 活性，并且改善抗炎活性，对 IFN-γ，IL-1β，IL-6 和 TNF-α 的 IC₅₀s 分别为 2.7 μM，2.9 μM，2.66 μM 和 2.66 μM。

生物活性

T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC₅₀s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.

体外研究

T6167923 (0-500 μM; 20 h) inhibits the pro-inflammatory cytokine response of staphylococcal enterotoxin B (SEB) in peripheral blood mono nuclear cells.
T6167923 (10-500 μM; 2 h) inhibits secreted alkaline phosphatase response (SEAP) expression in HEK 293T cells.
T6167923 (100 μM; 16 h) binds to TIR protein and reduced the inhibitory effect on MyD88-signaling.
T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation.

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

Cell Viability Assay

Cell Line:	Peripheral blood mono nuclear cells
Concentration:	0-500 μM
Incubation Time:	20 hours
Result:	Dose-dependently attenuated the response of SEB to TNF-α, INF-γ, IL-6, and IL-1β with IC₅₀s of 2.66, 2.7, 2.66 and 2.9 μM in peripheral blood mono nuclear cells.

Cell Viability Assay

Cell Line:	HEK 293T cell line
Concentration:	10-500 μM
Incubation Time:	2 hours
Result:	Dose-dependently inhibited lipo-polysaccharide (LPS) induced MyD88-mediated NF-kB driven SEAP expression in HEK 293T cells with IC₅₀s in the range of 40–50 μM.

Cell Viability Assay

Cell Line:	HEK 293T cell line
Concentration:	100 μM
Incubation Time:	16 hours
Result:	Specifically targeted MyD88 and dose-denpendently with TIR protein to reduced the inhibitory effect of MyD88-signaling.

Western Blot Analysis

Cell Line:	HEK 293-I3A cells with MyD88 knockout
Concentration:	1-500 μM
Incubation Time:	13 hours
Result:	Dose-dependently inhibited TIR domain-mediated dimerization of full-length MyD88 and the recombinant TIR domain protein.

体内研究
(In Vivo)

T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection.

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

Animal Model:	16-20 week-old BALB/c mice with LPS potentiation model
Dosage:	0.17 and 1 mg
Administration:	Intraperitoneal injection; 0.17 and 1 mg once
Result:	Dose-dependently showed a therapeutic efficacy against SEB intoxication.

体内研究

T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection.

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

Animal Model:	16-20 week-old BALB/c mice with LPS potentiation model
Dosage:	0.17 and 1 mg
Administration:	Intraperitoneal injection; 0.17 and 1 mg once
Result:	Dose-dependently showed a therapeutic efficacy against SEB intoxication.

体内研究

T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection.

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

Animal Model:	16-20 week-old BALB/c mice with LPS potentiation model
Dosage:	0.17 and 1 mg
Administration:	Intraperitoneal injection; 0.17 and 1 mg once
Result:	Dose-dependently showed a therapeutic efficacy against SEB intoxication.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (545.39 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1815 mL	10.9077 mL	21.8155 mL
5 mM	0.4363 mL	2.1815 mL	4.3631 mL
10 mM	0.2182 mL	1.0908 mL	2.1815 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 (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 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 (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 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 (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 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。