2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. ASB14780

ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM.

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

ASB14780 Chemical Structure

ASB14780 Chemical Structure

CAS No. : 1069046-00-9

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5 mg USD 140 In-stock
10 mg USD 225 In-stock
25 mg USD 450 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ASB14780 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM[1].

IC50 & Target

IC50: 20 nM (cPLA2α); 0.54 μM (guinea pig cPLA2α); 0.64 μM (human cPLA2α)[1]
In Vitro

ASB14780 shows selectivity to cPLA2α (IC50 =20 nM) over type II sPLA2 (IC50 >10 μM)[1].
ASB14780 (30 min pre-incucation) inhibits cPLA2α in guinea pig whole blood (GWB) and human whole blood (HWB) in a species-derived differences, with IC50s of 0.54 μM and 0.64 μM, respectively, 15 min after being stimulated by 5 μM calcium ionophore A23187[1].

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

ASB14780 Related Antibodies
In Vivo

TPA (tetradecanoyl phorbol acetate) causes acute inflammation with ear, resulting in edema[1].
ASB14780 (50 mg/kg; p.o.; once) suppresses the increase in the ear thickness elicited by the application of TPA (tetradecanoyl phorbol acetate) in mouse[1].
ASB14780 (5 mg/kg; 20 mg/kg; p.o.; once daily) attenuates AHR (airway hyperreactivity), and inhibits IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner[1].
ASB14780 shows well oral activity of 89.6% in mouse calculated from the ratio of oral administration’s AUC (10 mg/kg; p.o.) and intravenonous administration’s AUC (1 mg/kg; i.v.)[1].
Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780[1]

Model F (%) AUC (h?μg/mL) Cmax (μg/mL)
mouse 89.6 7.12 5.12
dog 34.3 17.1 4.96
monkey 30.9 4.96 2.29
Note: Based on 10 mg/kg p.o. dosing data.

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

Animal Model: TPA (Tetradecanoyl Phorbol Acetate)-induced Ear Edema Model in mouse (female C57BL/6 mice)[1]
Dosage: 50 mg/kg
Administration: Oral gavage; 30 min before TPA stimulation
Result: Showed high potency and inhibited ear swelling by 30% and indicated the in vivo anti-inflammatory activity.
Animal Model: Guinea Pig Ovalbumin (OVA)-induced Asthma Model[1]
Dosage: 5 mg/kg, 20 mg/kg
Administration: Oral gavage; two single doses; 1 h before and 8 h after passively sensitized administration
Result: Exhibits suppression on IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.
Molecular Weight

582.69

Formula

C35H38N2O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCC1=CC(C(CCC2=CC=CC=C2)=CN3C4=CC=C(C=C4)OC5=CC=CC=C5)=C3C=C1)O.OCC(CO)(CO)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (171.62 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 1.7162 mL 8.5809 mL 17.1618 mL
5 mM 0.3432 mL 1.7162 mL 3.4324 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). 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

×
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: ≥ 2.5 mg/mL (4.29 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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)

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). 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 1.7162 mL 8.5809 mL 17.1618 mL 42.9045 mL
5 mM 0.3432 mL 1.7162 mL 3.4324 mL 8.5809 mL
10 mM 0.1716 mL 0.8581 mL 1.7162 mL 4.2904 mL
15 mM 0.1144 mL 0.5721 mL 1.1441 mL 2.8603 mL
20 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
25 mM 0.0686 mL 0.3432 mL 0.6865 mL 1.7162 mL
30 mM 0.0572 mL 0.2860 mL 0.5721 mL 1.4301 mL
40 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
50 mM 0.0343 mL 0.1716 mL 0.3432 mL 0.8581 mL
60 mM 0.0286 mL 0.1430 mL 0.2860 mL 0.7151 mL
80 mM 0.0215 mL 0.1073 mL 0.2145 mL 0.5363 mL
100 mM 0.0172 mL 0.0858 mL 0.1716 mL 0.4290 mL
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ASB14780 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:

ASB147801069046-00-9ASB 14780ASB-14780Phosphataseimmediate asthmatic responseIAROvalbuminOVAAsthmalate asthmatic responseLARairway hyperreactivityAHRTXB 2Inhibitorinhibitorinhibit

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