1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. MD2-IN-1

MD2-IN-1 是髓样分化蛋白 2 (MD2) 的抑制剂,对重组人 MD2 (rhMD2) 的 KD 值为 189 μM。

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MD2-IN-1 Chemical Structure

MD2-IN-1 Chemical Structure

CAS No. : 111797-22-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2470
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1 mg ¥800
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5 mg ¥2250
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10 mg ¥3600
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25 mg ¥6500
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查看 Toll-like Receptor (TLR) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189  μM for the recombinant human MD2 (rhMD2).

IC50 & Target

KD: 189 μM (rhMD2)[1]

体外研究
(In Vitro)

Myeloid differentiation protein 2 (MD2) is a co-receptor of TLR4. Among those derivatives, MD2-IN-1 (compound 20) shows the strongest inhibitory effect on LPS-induced expression of both TNF-α and IL-6. Compare to the vehicle, LPS alone largely increases the amount of TLR4/MD2 complex, while pretreatment with MD2-IN-1 inhibits the increase of TLR4/MD2 complex to the vehicle level. SPR analysis shows that MD2-IN-1 exhibits recognizable binding to rhMD2 protein in a dose-dependent manner, with a KD value of 189 μM, while the KD value of xanthohumol binding to MD2 is 460 μM. Pre-treatment with different doses of MD2-IN-1 dose-dependently reduces FITC-LPS binding to MD2 in cell surface membranes, with a 65% inhibition at 10 μM in terms of mean fluorescence intensity. Pretreatment with MD2-IN-1 also dose-dependently blocks LPS-induced MAPK phosphorylation in the MPMs[1].

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

体内研究
(In Vivo)

Administration of MD2-IN-1 evidently reduces the LPS-induced increase in protein concentrations in BALF. The lung wet/dry weight ratio is markedly higher in the LPS-treated group than the control group, and MD2-IN-1 treatment reduces LPS-induced pulmonary edema. LPS also causes observable lung histopathologic changes, including areas of inflammatory infiltration, hemorrhage, interstitial edema, thickening of the alveolar wall, and lung tissue destruction. These histopathological changes are ameliorated in the MD2-IN-1 treatment group[1].

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

分子量

358.39

Formula

C20H22O6

CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (139.51 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.25 mg/mL (9.07 mM); 澄清溶液

    此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3.25 mg/mL (9.07 mM); 悬浊液; 超声助溶

    此方案可获得 3.25 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 32.5 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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.89%

参考文献
Cell Assay
[1]

Mouse RAW264.7 macrophages are starved for 3 h before experimentation. Cells are incubated with or without FITC-LPS (50 μg/mL) in the presence or absence of MD2-IN-1 (0.1, 1 and 10 μM) for 30 min. After incubation, macrophages are fixed with paraformaldehyde for 10 min at 4°C and washed with PBS before being analyzed by flow cytometry[1].

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

Animal Administration
[1]

Male Sprague Dawley (SD) rats are randomly divided into three groups, designated “control” (5 rats, only receive the vehicle of 0.9% saline), “LPS” (7 rats, receive 5 mg/kg LPS alone) and “MD2-IN-1 (20) + LPS” (6 rats, receive both MD2-IN-1 and 5 mg/kg LPS). Prior to LPS-induced Acute lung injury (ALI), the MD2-IN-1+LPS group rats are treated intragastrically with MD2-IN-1 at a dosage of 20 mg/kg/day continuously for one week. Under ether anesthesia, all the rats are exposed their trachea and challenged with intratracheal instillation of 50 μL of LPS, while the control group challenged with intratracheal instillation of 50 μL of 0.9% saline. Rats are then euthanized with ketamine after 6 h of LPS induction[1].

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

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7903 mL 13.9513 mL 27.9026 mL 69.7564 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL 13.9513 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL 6.9756 mL
15 mM 0.1860 mL 0.9301 mL 1.8602 mL 4.6504 mL
20 mM 0.1395 mL 0.6976 mL 1.3951 mL 3.4878 mL
25 mM 0.1116 mL 0.5581 mL 1.1161 mL 2.7903 mL
30 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3252 mL
40 mM 0.0698 mL 0.3488 mL 0.6976 mL 1.7439 mL
50 mM 0.0558 mL 0.2790 mL 0.5581 mL 1.3951 mL
60 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1626 mL
80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8720 mL
100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6976 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MD2-IN-1
目录号:
HY-103483
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