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  3. WWL70

WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.

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WWL70 Chemical Structure

WWL70 Chemical Structure

CAS No. : 947669-91-2

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Based on 2 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.

IC50 & Target

IC50: 70 nM (ABHD6)[1]

In Vitro

At 1 h after WWL70 (10 μM) treatment, 2-Arachidonoylglycerol (2-AG) is increased by 20% compare to untreated cells. At either 1 or 10 μM, WWL70 completely blocks the lipopolysaccharide (LPS)-induced increase of PGE2. The enhanced mRNA expression of mPGES-1 and mPGES-2 by LPS is also reduced by WWL70. The IC50 of WWL70 to inhibit the PGE2 biosynthesis is about 100 nM[2].

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

In Vivo

Although post-treatment with WWL70 at 5 mg/kg does not have any effect, treatment with WWL70 at 10 mg/kg improves the performance significantly. WWL70 treatment improves motor coordination of traumatic brain injury (TBI) mice in a concentration dependent manner. The latency to fall in animals treated with WWL70 at 5 mg/kg increases from 74.92±4.8 to 99.57±5.21 on day 3 (p<0.01) and from 87.32±4.42 to 100.14±3.56 on day 7 (p<0.05) post-injury when compare with the vehicle-TBI groups. At 10 mg/kg, WWL70 treatment improves motor coordination starting on day 1 post-injury. WWL70 treatment completely restores the ability of TBI mice to continuously alternate arms during Y maze exploration (69.67±4.98 %)[3].

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

Molecular Weight

437.49

Formula

C27H23N3O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OC1=CC=C(C2=CC=C(C(N)=O)C=C2)C=C1)N(C)CC3=CC=CC(C4=CC=NC=C4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 17.33 mg/mL (39.61 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 2.2858 mL 11.4288 mL 22.8577 mL
5 mM 0.4572 mL 2.2858 mL 4.5715 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.95%

References
Kinase Assay
[2]

One hundred micrograms per milliliter of BV2 microsomes are pre-incubated with WWL70 for 5 min at 23°C, then mixed with 10 μM of Arachidonic acid (AA) for 1 min at 23°C. 500 μg/mL brain microsomes are incubated with 10 μM of AA for 2 min at 23°C. The reaction is stopped by mixing with stannous acid (5 mg/mL in 0.1 N HCl) to deactivate the enzyme and convert intermediate PGH2 to PGF, followed by the measurement of PGE2 concentration by Enzyme-linked immunoassay (EIA). The activity is determined after subtraction with the amount of PGE2 in the microsome fraction incubated without substrate[2].

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

Cell Assay
[2]

BV2 cells (90% confluence) in 10-cm dishes are treated with WWL70 (10 μM) for 1 h. After rinsing with PBS once, the cells are collected by centrifugation at 5000 g for 2 min. The pellet is suspended with 0.1 mL of 0.02% trifluoroacetic acid (TFA) and 1 nmol of 2-AG-d8 by pipetting and dispersed in 4 mL of acetonitrile in a silanized glass tube to precipitate the debris overnight at -20°C. The supernatant after centrifuged at 5000 g for 5 min is transferred to a new glass tube and evaporated under a nitrogen gas stream in a mild hot water bath (approximately 35°C). 2-AG is resuspended with 0.1 mL of acetonitrile and stored at -80°C until mass analysis[2].

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

Animal Administration
[3]

Seven-week-old, male C57BL/6 mice weighing 25 to 30 g are used in this study. Animals are maintained under a controlled environment with a temperature of 23±2°C, a 12 h light/dark cycle, and access to food and water ad libitum. WWL70 (5 mg/kg or 10 mg/kg) in physiologic saline or an equal volume of 1% DMSO in saline (10 mL/kg) is injected intraperitoneally, and then once a day for 3, 7, or 21 days depending on the experimental design. During the 21-day treatment regimen, animals are subjected to a battery of behavioral tests at different time points. Two hours after the last injection on day 21 post-injury, animals are sacrificed and brain tissues are collected for histological analysis[3].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2858 mL 11.4288 mL 22.8577 mL 57.1442 mL
5 mM 0.4572 mL 2.2858 mL 4.5715 mL 11.4288 mL
10 mM 0.2286 mL 1.1429 mL 2.2858 mL 5.7144 mL
15 mM 0.1524 mL 0.7619 mL 1.5238 mL 3.8096 mL
20 mM 0.1143 mL 0.5714 mL 1.1429 mL 2.8572 mL
25 mM 0.0914 mL 0.4572 mL 0.9143 mL 2.2858 mL
30 mM 0.0762 mL 0.3810 mL 0.7619 mL 1.9048 mL
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  • 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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