2. Immunology/Inflammation
  3. PGE synthase
  4. mPGES1-IN-7

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice.

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mPGES1-IN-7 Chemical Structure

mPGES1-IN-7 Chemical Structure

CAS No. : 1268709-57-4

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Based on 1 publication(s) in Google Scholar

mPGES1-IN-7 Related Antibodies

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  • Purity & Documentation

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Description

mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice[1].

IC50 & Target

IC50: 0.9 μM (recombinant human mPGES-1), 0.09 μM (recombinant rat mPGES-1)[1]; lipocalin-type PGD synthase (I-PGDS)[1]
In Vitro

mPGES-1-IN-2 (compound III) (0.64-80 μM; 24 h) can reduce PGE2 production after LPS (10 ng/mL) stimulation in A549 cells, mouse macrophages, and blood [1] .br/mPGES-1-IN-2 () Inhibits PGE2 synthesis in a concentration-dependent manner, causing PGH2 to shunt to the prostacyclin pathway[1].

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

mPGES1-IN-7 Related Antibodies
In Vivo

mPGES-1-IN-2 (compound III) (10-100 mg/kg; ip; single dose) effectively inhibits global prostaglandin production in a mouse model of air sac inflammation induced by 1% λ-Carrageenan (HY-N9470). synthesis and reduce cell migration[1].

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

Animal Model: 1% Carrageenan stimulated mouse air pouch model[1]
Dosage: 10, 50, 100 mg/kg
Administration: ip; single dose after modeling: use 3 mL of sterile-filtered air was injected sub-cutaneously into the interscapular region of mice; triggered in the pouch 24 h later by the injection of a 1 ml solution of λ-carrageenan (1%) in saline.
Result: Had no effect on inflammatory exudate volume but dose-dependently reduced cell migration.
Resulted in a decrease in PGE2 synthesis, it does not affect changes in other prostaglandin levels, but leads to an overall downregulation of prostaglandin synthesis.
Molecular Weight

382.54

Formula

C23H34N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1CCCC1)C2CCN(CC2)C3=NC4=CC(C)=C(C=C4N3C(C)C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (87.13 mM; ultrasonic and warming and heat to 60°C; 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 2.6141 mL 13.0705 mL 26.1411 mL
5 mM 0.5228 mL 2.6141 mL 5.2282 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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: ≥ 2 mg/mL (5.23 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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.
Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6141 mL 13.0705 mL 26.1411 mL 65.3526 mL
5 mM 0.5228 mL 2.6141 mL 5.2282 mL 13.0705 mL
10 mM 0.2614 mL 1.3071 mL 2.6141 mL 6.5353 mL
15 mM 0.1743 mL 0.8714 mL 1.7427 mL 4.3568 mL
20 mM 0.1307 mL 0.6535 mL 1.3071 mL 3.2676 mL
25 mM 0.1046 mL 0.5228 mL 1.0456 mL 2.6141 mL
30 mM 0.0871 mL 0.4357 mL 0.8714 mL 2.1784 mL
40 mM 0.0654 mL 0.3268 mL 0.6535 mL 1.6338 mL
50 mM 0.0523 mL 0.2614 mL 0.5228 mL 1.3071 mL
60 mM 0.0436 mL 0.2178 mL 0.4357 mL 1.0892 mL
80 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8169 mL
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mPGES1-IN-7 Related Classifications

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:

mPGES1-IN-71268709-57-4PGE synthaseProstaglandin E synthaseAir pouch modelInflammationMacrophagesMousePGE2mPGES-1Inhibitorinhibitorinhibit

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