1. Metabolic Enzyme/Protease
  2. Phospholipase
  3. sPLA2 inhibitor 1

sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.

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sPLA2 inhibitor 1 Chemical Structure

sPLA2 inhibitor 1 Chemical Structure

CAS No. : 393569-31-8

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500 μg USD 45 In-stock
1 mg USD 70 In-stock
5 mg USD 260 In-stock
10 mg USD 450 In-stock
25 mg USD 890 In-stock
50 mg USD 1420 In-stock
100 mg USD 2200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity[1].

IC50 & Target[1]

sPLA2

29 nM (IC50)

In Vivo

sPLA2 inhibitor 1 (compound 2b; oral; 5 mg/kg/day; on Days 10-13 after inoculation with arthritogen) shows substantial inhibition of the oedema. Drug-treated rats shows mild capsular oedema and minimal infiltration of macrophages into the red pulp[1].

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

Molecular Weight

487.63

Formula

C31H37NO4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(CC[C@@H](CC1=CC=C(OCC2=CC=CC=C2)C=C1)NC(CCCCCCC3=CC=CC=C3)=O)=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 : 100 mg/mL (205.07 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 2.0507 mL 10.2537 mL 20.5074 mL
5 mM 0.4101 mL 2.0507 mL 4.1015 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
×
Volume
×
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: 2.5 mg/mL (5.13 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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 (25.0 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 2.0507 mL 10.2537 mL 20.5074 mL 51.2684 mL
5 mM 0.4101 mL 2.0507 mL 4.1015 mL 10.2537 mL
10 mM 0.2051 mL 1.0254 mL 2.0507 mL 5.1268 mL
15 mM 0.1367 mL 0.6836 mL 1.3672 mL 3.4179 mL
20 mM 0.1025 mL 0.5127 mL 1.0254 mL 2.5634 mL
25 mM 0.0820 mL 0.4101 mL 0.8203 mL 2.0507 mL
30 mM 0.0684 mL 0.3418 mL 0.6836 mL 1.7089 mL
40 mM 0.0513 mL 0.2563 mL 0.5127 mL 1.2817 mL
50 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0254 mL
60 mM 0.0342 mL 0.1709 mL 0.3418 mL 0.8545 mL
80 mM 0.0256 mL 0.1282 mL 0.2563 mL 0.6409 mL
100 mM 0.0205 mL 0.1025 mL 0.2051 mL 0.5127 mL
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sPLA2 inhibitor 1 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.

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sPLA2 inhibitor 1
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