2. Immunology/Inflammation
  3. PGE synthase
  4. Vipoglanstat

Vipoglanstat  (Synonyms: BI 1029539; GS-248; OX-MPI)

Cat. No.: HY-147416 Purity: 99.74%
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Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity.

For research use only. We do not sell to patients.

Vipoglanstat Chemical Structure

Vipoglanstat Chemical Structure

CAS No. : 1360622-01-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 866 In-stock
Solution
10 mM * 1 mL in DMSO USD 866 In-stock
Solid
5 mg USD 580 In-stock
10 mg USD 1050 In-stock
25 mg USD 2250 In-stock
50 mg USD 3600 In-stock
100 mg USD 5800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Vipoglanstat Related Antibodies

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Description

Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity[1][2].

In Vitro

Vipoglanstat significantly inhibits mPGES-1 level (IC50: about 1 nM)[3].
Vipoglanstat blocks the up-regulation of P-gp and mPGES-1 levels on glutamate-mediatedin isolated brain capillaries[3].
Vipoglanstat reduces human peripheral blood inflammatory cell migration and inflammatory mediator release[3].

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

Vipoglanstat Related Antibodies
In Vivo

Vipoglanstat (30 mg/kg; i.p.) can reduce LPS-induced lung injury, with reduction in neutrophil influx, protein content, TNF-ɑ, IL-1β and PGE2 levels in bronchoalveolar lavage (BAL), myeloperoxidase activity, expression of mPGES-1, cyclooxygenase (COX)-2 and intracellular adhesion molecule in lung tissue[2].
Vipoglanstat (30 mg/kg; p.o.; 2 h, 8 h and 22 h) significantly reduces sepsis-induced BAL inflammatory cell recruitment, lung injury score and lung expression of mPGES-1 and inducible nitric oxide synthase[2].
Vipoglanstat (30 mg/kg; p.o.; QD) also significantly prolongs survival of mice with severe sepsis[2].

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

Animal Model: LPS-induced acute lung injury models[2]
Dosage: 30 mg/kg
Administration: 30 mg/kg, i.p.
Result: Preserved lung architecture and reduced immune cell influx into the lungs of LPS‑challenged mice.
Animal Model: CLP-induced sepsis models[2]
Dosage: 30 mg/kg
Administration: 30 mg/kg, p.o., 2 hrs, 8 hrs and 22 hrs; 30 mg/kg, p.o., QD
Result: Attenuated CLP‑induced lung injury and prolongs survival.
Clinical Trial
Molecular Weight

678.52

Formula

C30H34Cl2F5N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN1C2=CC(OCC(F)F)=C(C(N[C@@H]3CC[C@H](CC3)C(F)(F)F)=O)C=C2N=C1NC4=C(C(CNC(C(C)(C)C)=O)=CC=C4Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (221.07 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 1.4738 mL 7.3690 mL 14.7380 mL
5 mM 0.2948 mL 1.4738 mL 2.9476 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 (sealed storage, away from moisture and light). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% Corn Oil

    Solubility: ≥ 3.75 mg/mL (5.53 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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 (sealed storage, away from moisture and light). 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 1.4738 mL 7.3690 mL 14.7380 mL 36.8449 mL
5 mM 0.2948 mL 1.4738 mL 2.9476 mL 7.3690 mL
10 mM 0.1474 mL 0.7369 mL 1.4738 mL 3.6845 mL
15 mM 0.0983 mL 0.4913 mL 0.9825 mL 2.4563 mL
20 mM 0.0737 mL 0.3684 mL 0.7369 mL 1.8422 mL
25 mM 0.0590 mL 0.2948 mL 0.5895 mL 1.4738 mL
30 mM 0.0491 mL 0.2456 mL 0.4913 mL 1.2282 mL
40 mM 0.0368 mL 0.1842 mL 0.3684 mL 0.9211 mL
50 mM 0.0295 mL 0.1474 mL 0.2948 mL 0.7369 mL
60 mM 0.0246 mL 0.1228 mL 0.2456 mL 0.6141 mL
80 mM 0.0184 mL 0.0921 mL 0.1842 mL 0.4606 mL
100 mM 0.0147 mL 0.0737 mL 0.1474 mL 0.3684 mL
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Vipoglanstat 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:

Vipoglanstat1360622-01-0BI 1029539 GS-248 OX-MPIBI1029539BI-1029539GS248GS 248GS-248PGE synthaseProstaglandin E synthasemPGEScarboxamideoralanti-inflammatoryhuman prostaglandin E synthase 1(mPGES-1)Inhibitorinhibitorinhibit

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