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

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

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MD2-IN-1

MD2-IN-1 構造式

CAS 番号 : 111797-22-9

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 174 在庫あり
Solution
10 mM * 1 mL in DMSO USD 174 在庫あり
Solid
5 mg $159 在庫あり
10 mg $238 在庫あり
25 mg $452 在庫あり
50 mg $680 在庫あり
100 mg $1020 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 7 publication(s) in Google Scholar

Other Forms of MD2-IN-1:

MD2-IN-1 関連抗体

Top Publications Citing Use of Products

Toll-like Receptor (TLR) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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

TLR4

 

Cellular Effect
Cell Line Type Value Description References
K562 IC50
1.1 μM
Compound: 2q
Antiproliferative activity against human K562 cells after 5 days by MTT assay
Antiproliferative activity against human K562 cells after 5 days by MTT assay
[PMID: 19837593]
MCF7 GI50
3.97 μM
Compound: 18
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by sulforhodamine B assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by sulforhodamine B assay
[PMID: 31610374]
NCI-H460 GI50
5.6 μM
Compound: 18
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by sulforhodamine B assay
[PMID: 31610374]
RAW264.7 IC50
12.3 μM
Compound: 3l
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-1beta release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-1beta release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
[PMID: 38911149]
RAW264.7 IC50
2.1 μM
Compound: 3l
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of IL-6 release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
[PMID: 38911149]
RAW264.7 IC50
4 μM
Compound: 3l
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of PGE2 production preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of PGE2 production preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
[PMID: 38911149]
RAW264.7 IC50
4.6 μM
Compound: 3l
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of iNOS activity preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of iNOS activity preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
[PMID: 38911149]
RAW264.7 IC50
7.9 μM
Compound: 3l
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of TNF-alpha release preincubated for 2 hrs followed by LPS stimulation for 24 hrs by ELISA method
[PMID: 38911149]
体外実験

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].

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

MD2-IN-1 関連抗体
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

358.39

分子式

C20H22O6
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(OC)C(OC)=C1)/C=C/C2=CC(OC)=C(OC)C(OC)=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (139.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
10 mM 0.2790 mL 1.3951 mL 2.7903 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.25 mg/mL (9.07 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3.25 mg/mL (9.07 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献
細胞実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 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
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MD2-IN-1 Related Classifications

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

MD2-IN-1111797-22-9Toll-like Receptor (TLR)Inhibitorinhibitorinhibit

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製品名:
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製品番号:
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