[CAS NO. 947669-86-5] WWL113
PRODUCTS SPECIFICATIONS [947669-86-5]
DESCRIPTION [947669-86-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 466.53 |
| Molecular Formula | C29H26N2O4 |
| SMILES | CN(CC1=CC(C2=CC=NC=C2)=CC=C1)C(OC3=CC=C(C4=CC=C(C(OCC)=O)C=C4)C=C3)=O |
Summary
WWL113 is a selective and orally active Ces3 and Ces1f inhibitor, with IC 50 values of 120 nM and 100 nM for Ces3 and Ces1f, respectively. WWL113 appears to show excellent selectivity for the 60-kDa serine hydrolase (or hydrolases) [1] .
IC50 & Target
IC50: 120 nM (Ces3), 100 nM (Ces1f) [1] .
In Vitro
Ces3 and Ces1f are endoplasmic reticulum glycoproteins that have been previously associated with adipocyte lipolysis. WWL113 inhibits mouse recombinant Ces1, Ces1c, and ABHD6 at 10 μM
[1]
.
WWL113 (1 μM) significantly increases UCP1 protein expression in brown adipocytes
[2]
.
WWL113 has a partial, statistically significant inhibitory effect on blocking the buildup of PGE2
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
WWL113 (30 mg/kg, orally once a day) results in major improvement of multiple features of metabolic syndrome and ameliorated obesity-diabetes in mice with lowered levels of nonesterified free fatty acids (NEFAs), triglycerides (TGs), total cholesterol and fasted glucose as well as enhanced glucose tolerance
[1]
.
WWL113 ameliorates obesity-diabetes in mice
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Eight-week-old db/db mice (n = 10 per group) [1] . |
| Dosage: | 30 mg/kg. |
| Administration: | Orally once a day for 3 weeks. |
| Result: | Corrected multiple features of metabolic syndrome in db/db mice. |
Appearance
Solid
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
DMSO : 20.83 mg/mL ( 44.65 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1435 mL | 10.7174 mL | 21.4348 mL |
| 5 mM | 0.4287 mL | 2.1435 mL | 4.2870 mL |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1435 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution
References
- [1] Dominguez, E., Galmozzi, A., Chang, J.W., et al. Integrated phenotypic and activity-based profiling links Ces3 to obesity and diabetes. Nat. Chem. Biol. 10(2), 113-121 (2014).
- [2] Galmozzi, et al. ThermoMouse: an in vivo model to identify modulators of UCP1 expression in brown adipose tissue. Cell Rep. 2014 Dec 11;9(5):1584-1593.
- [3] Turcotte C, et al. The Endocannabinoid Metabolite Prostaglandin E2 (PGE2)-Glycerol Inhibits Human Neutrophil Functions: Involvement of Its Hydrolysis into PGE2 and EP Receptors. J Immunol. 2017 Apr 15;198(8):3255-3263.