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MD2-IN-1

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Catalog No. T4231Cas No. 111797-22-9

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

MD2-IN-1

MD2-IN-1

🥰Excellent
Purity: 99.43%
Catalog No. T4231Cas No. 111797-22-9
MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).
Pack SizePriceAvailabilityQuantity
1 mg$54In Stock
5 mg$128In Stock
10 mg$196In Stock
25 mg$373In Stock
50 mg$562In Stock
100 mg$845In Stock
1 mL x 10 mM (in DMSO)$142In Stock
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Purity:99.43%
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Product Introduction

Bioactivity
Description
MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).
Targets&IC50
MD2 (recombinant human):189 μM (KD)
In vitro
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. Compared 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.
In vivo
In the LPS-treated group, the lung wet/dry weight ratio significantly exceeds that of controls, indicating LPS-induced pulmonary edema, which MD2-IN-1 treatment effectively mitigates. Additionally, MD2-IN-1 markedly lowers the elevated protein levels in BALF caused by LPS. LPS administration results in noticeable lung histopathological alterations, such as inflammatory infiltration, hemorrhage, interstitial edema, alveolar wall thickening, and lung tissue destruction, all of which are significantly improved with MD2-IN-1 treatment.
Cell Research
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.
Animal Research
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.
Chemical Properties
Molecular Weight358.39
FormulaC20H22O6
Cas No.111797-22-9
SmilesCOc1ccc(cc1OC)C(=O)\C=C\c1cc(OC)c(OC)c(OC)c1
Relative Density.1.156 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (153.46 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7903 mL13.9513 mL27.9026 mL139.5128 mL
5 mM0.5581 mL2.7903 mL5.5805 mL27.9026 mL
10 mM0.2790 mL1.3951 mL2.7903 mL13.9513 mL
20 mM0.1395 mL0.6976 mL1.3951 mL6.9756 mL
50 mM0.0558 mL0.2790 mL0.5581 mL2.7903 mL
100 mM0.0279 mL0.1395 mL0.2790 mL1.3951 mL

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