BI 78D3|883065-90-5|-陌孚医药/Medlife

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BI 78D3

目录号: PC11833 纯度: ≥98%

CAS No. :883065-90-5

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PC11833-5mg	5mg	¥1034.88	请登录
PC11833-10mg	10mg	¥1587.60	请登录
PC11833-25mg	25mg	¥3351.60	请登录
PC11833-100mg	100mg	¥9525.60	请登录
PC11833-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1138.76	请登录

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中文名称

BI 78D3

中文别名

4-(2,3-二氢-1,4-苯并二恶英-6-基)-2,4-二氢-5-[(5-硝基-2-噻唑基)硫基]-3H-1,2,4-三唑-3-酮;4-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-2,4-DIHYDRO-5-[(5-NITRO-2-THIAZOLYL)THIO]-3H-1,2,4-TRIAZOL-3-ONE

英文名称

BI 78D3

英文别名

4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-3-((5-nitrothiazol-2-yl)thio)-1H-1,2,4-triazol-5(4H)-one;4-(2,3-DIHYDRO-1,4-BENZODIOXIN-6-YL)-2,4-DIHYDRO-5-[(5-NITRO-2-THIAZOLYL)THIO]-3H-1,2,4-TRIAZOL-3-ONE;4-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[(5-nitro-1,3-thiazol-2-yl)sulfanyl]-1H-1,2,4-triazol-5-one;4-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-3-((5-nitro-thiazol-2-yl)thio)-1H-1,2,4-triazol-5(4H)-one;BI 78D3;BI-78D3;4-(2,3-Dihydrobenzol[b][1,4]dioxin-6-yl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol;4-(2,3-dihydro-1,4-benzodioxin-6-yl)-3-[(5-nitro-2-thiazolyl)thio]-1H-1,2,4-triazol-5-one;MLS006010634;BDBM26057

Cas No.

883065-90-5

分子式

C₁₃N₅O₅S₂H₉

分子量

379.37

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC₅₀=280 nM).

性状

Solid

IC50 & Target[1][2]

JNK

280 nM (IC₅₀)

体外研究(In Vitro)

BI-78D3, dose-dependently inhibits the phosphorylation of JNK substrates both 体外研究 and in cell. BI-78D3 is able to compete with the D-domain of JIP1 (amino acids 153-163; pepJIP1) for JNK1 binding (IC₅₀=500 nM). Using the same 体外研究 LanthaScreen kinase assay and the same ATF2 substrate, BI-78D3 is found to be 100-fold less active vs. p38α, a member of the MAPK family with high structural similarity to JNK, and completely inactive against mTOR and PI3-kinase (α-isoform), both unrelated protein kinases. Furthermore, Lineweaver-Burk analysis clearly indicates that BI-78D3 is competitive with ATF2 for binding to JNK1 with an apparent K_i value of 200 nM. In an attempt to profile the properties of BI-78D3 in the context of a complex cellular milieu, the cell-based LanthaScreen kinase assay is used. In this assay BI-78D3 is able to inhibit TNF-α stimulated phosphorylation of c-Jun in cell (EC₅₀=12.4 μM).

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

体内研究(In Vivo)

The link between ConA-induced liver failure, TNF receptor signaling, and JNK function has been established by studies employing JNK1 and JNK2 mice. For this analysis, insulin insensitive mice are injected only once with 25 mg/kg BI-78D3, 30 min before insulin injection. The effect of insulin on blood glucose levels is then measured. BI-78D3 results in a statistically significant reduction in blood glucose levels as compared with the vehicle control. Thus, the ability of BI-78D3 to abrogate ConA-induced liver damage and restore insulin sensitivity is consistent with its proposed function as an effective JNK inhibitor. Liquid chromatography/mass spectrometry bio-availability analysis demonstrates that BI-78D3 has favorable microsome and plasma stability (T_1/2=54 min).

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

运输条件

Room temperature or refrigerated transportation.

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

[1]. Stebbins JL et al. Identification of a new JNK inhibitor targeting the JNK-JIP interaction site. Proc Natl Acad Sci U S A, 2008 Oct 28, 105(43):16809-13. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (263.59 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6359 mL	13.1797 mL	26.3595 mL
5 mM	0.5272 mL	2.6359 mL	5.2719 mL
10 mM	0.2636 mL	1.3180 mL	2.6359 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.59 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 ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.59 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 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

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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