2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. Lp-PLA2-IN-3

Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2).

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

Lp-PLA2-IN-3 Chemical Structure

Lp-PLA2-IN-3 Chemical Structure

CAS No. : 2196245-16-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 298 In-stock
Solution
10 mM * 1 mL in DMSO USD 298 In-stock
Solid
5 mg USD 290 In-stock
10 mg USD 460 In-stock
50 mg USD 1070 In-stock
100 mg USD 1450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Lp-PLA2-IN-3 Related Antibodies

Top Publications Citing Use of Products

View All Phospholipase Isoform Specific Products:

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Phospholipase A PLD Phospholipase C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Lp-PLA2-IN-3 is a potent and orally bioavailable lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 14 nM for recombinant human Lp-PLA2 (rhLpPLA2)[1].

In Vivo

Lp-PLA2-IN-3 (3 mg/kg; p.o.) treatment shows the Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 3.4 μg h/mL, 7.7 hours and 35.5%, respectively[1].
Lp-PLA2-IN-3 (1 mg/kg; i.v.) treatment shows the CL, Vss, and t1/2 were 3.1mL/min/kg, 0.3 L/kg, 4 hours, respectively[1].

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

Animal Model: Male Sprague−Dawley (SD) rats (180-220 g)[1]
Dosage: 3 mg/kg
Administration: p.o. (Pharmacokinetic Analysis)
Result: The Cmax, AUC0-24h, t1/2 and F were 0.27 μg/mL, 6.2 μg h/mL, 7.7 hours and 35.5%, respectively.
Molecular Weight

467.85

Formula

C20H13ClF3N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N)C=C1)(NC2=CC=C(OC3=CC=C(Cl)C(C(F)(F)F)=C3)C(C#N)=C2)=O
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 : ≥ 250 mg/mL (534.36 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1374 mL 10.6872 mL 21.3744 mL
5 mM 0.4275 mL 2.1374 mL 4.2749 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
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

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).
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 2.1374 mL 10.6872 mL 21.3744 mL 53.4359 mL
5 mM 0.4275 mL 2.1374 mL 4.2749 mL 10.6872 mL
10 mM 0.2137 mL 1.0687 mL 2.1374 mL 5.3436 mL
15 mM 0.1425 mL 0.7125 mL 1.4250 mL 3.5624 mL
20 mM 0.1069 mL 0.5344 mL 1.0687 mL 2.6718 mL
25 mM 0.0855 mL 0.4275 mL 0.8550 mL 2.1374 mL
30 mM 0.0712 mL 0.3562 mL 0.7125 mL 1.7812 mL
40 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3359 mL
50 mM 0.0427 mL 0.2137 mL 0.4275 mL 1.0687 mL
60 mM 0.0356 mL 0.1781 mL 0.3562 mL 0.8906 mL
80 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.6679 mL
100 mM 0.0214 mL 0.1069 mL 0.2137 mL 0.5344 mL
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Lp-PLA2-IN-3 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:

Lp-PLA2-IN-32196245-16-4PhospholipaseInhibitorinhibitorinhibit

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